Malcolm Stevens

Q: What Schools Are Affiliated With Malcolm Stevens

Malcolm Stevens is affiliated with the following schools: University of Nottingham, University of Oxford, Aston University

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Malcolm Stevens

Chemistry

#4482

World Rank

#5565

Historical Rank

Organic Chemistry

#788

World Rank

#887

Historical Rank

chemistry Degrees

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Chemistry

Malcolm Stevens's Degrees

PhD Chemistry University of Oxford
Bachelors Chemistry University of Oxford

Why Is Malcolm Stevens Influential?

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According to Wikipedia, Malcolm Francis Graham Stevens OBE, FRS is an English chemist and Emeritus professor of the University of Nottingham, having previously worked at Aston University where he developed the cancer drug temozolomide.

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Malcolm Stevens's Published Works

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Total number of citations to an author for the works they published in a given year. This highlights publication of the most important work(s) by the author

Published Works

Temozolomide: a review of its discovery, chemical properties, pre-clinical development and clinical trials. (1997) (720)
Temozolomide: mechanisms of action, repair and resistance. (2012) (605)
Phase I trial of temozolomide (CCRG 81045: M&B 39831: NSC 362856). (1992) (501)
Antitumor activity and pharmacokinetics in mice of 8-carbamoyl-3-methyl-imidazo[5,1-d]-1,2,3,5-tetrazin-4(3H)-one (CCRG 81045; M & B 39831), a novel drug with potential as an alternative to dacarbazine. (1987) (393)
Antitumor benzothiazoles. 26.(1) 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (GW 610, NSC 721648), a simple fluorinated 2-arylbenzothiazole, shows potent and selective inhibitory activity against lung, colon, and breast cancer cell lines. (2006) (389)
NMR and molecular modeling investigation of the mechanism of activation of the antitumor drug temozolomide and its interaction with DNA. (1994) (381)
Antitumor benzothiazoles. 16. Synthesis and pharmaceutical properties of antitumor 2-(4-aminophenyl)benzothiazole amino acid prodrugs. (2002) (380)
Antitumor benzothiazoles. 3. Synthesis of 2-(4-aminophenyl)benzothiazoles and evaluation of their activities against breast cancer cell lines in vitro and in vivo. (1996) (344)
Antitumor benzothiazoles. 14. Synthesis and in vitro biological properties of fluorinated 2-(4-aminophenyl)benzothiazoles. (2001) (317)
Cancer Research Campaign phase II trial of temozolomide in metastatic melanoma. (1995) (285)
Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (PMX 610, NSC 721648). (2008) (262)
Telomere damage induced by the G-quadruplex ligand RHPS4 has an antitumor effect. (2007) (219)
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles. (1999) (212)
Potent inhibition of telomerase by small-molecule pentacyclic acridines capable of interacting with G-quadruplexes. (2001) (197)
2-(4-Aminophenyl)benzothiazoles: novel agents with selective profiles of in vitro anti-tumour activity. (1998) (195)
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent. (1984) (188)
Telomere uncapping by the G-quadruplex ligand RHPS4 inhibits clonogenic tumour cell growth in vitro and in vivo consistent with a cancer stem cell targeting mechanism (2007) (172)
Drug recognition and stabilisation of the parallel-stranded DNA quadruplex d(TTAGGGT)4 containing the human telomeric repeat. (2003) (164)
Stabilization of quadruplex DNA perturbs telomere replication leading to the activation of an ATR-dependent ATM signaling pathway (2009) (154)
Biological Activity of the G-Quadruplex Ligand RHPS4 (3,11-Difluoro-6,8,13-trimethyl-8H-quino[4,3,2-kl]acridinium methosulfate) Is Associated with Telomere Capping Alteration (2004) (134)
Semisynthesis and in vitro anticancer activities of andrographolide analogues. (2007) (127)
Antitumor benzothiazoles. 7. Synthesis of 2-(4-acylaminophenyl)benzothiazoles and investigations into the role of acetylation in the antitumor activities of the parent amines. (1999) (120)
Antitumour 2-(4-aminophenyl)benzothiazoles generate DNA adducts in sensitive tumour cells in vitro and in vivo (2003) (113)
PARP1 is activated at telomeres upon G4 stabilization: possible target for telomere-based therapy (2010) (106)
Acquired Resistance to Temozolomide in Glioma Cell Lines: Molecular Mechanisms and Potential Translational Applications (2010) (105)
Role of Cyp1A1 in modulation of antitumor properties of the novel agent 2-(4-amino-3-methylphenyl)benzothiazole (DF 203, NSC 674495) in human breast cancer cells. (2000) (104)
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide. (1995) (103)
Antitumour benzothiazoles. Part 20: 3'-cyano and 3'-alkynyl-substituted 2-(4'-aminophenyl)benzothiazoles as new potent and selective analogues. (2003) (103)
Antitumor polycyclic acridines. 8.(1) Synthesis and telomerase-inhibitory activity of methylated pentacyclic acridinium salts. (2002) (101)
Antitumour properties of fluorinated benzothiazole-substituted hydroxycyclohexa-2,5-dienones ('quinols'). (2006) (100)
DNA damage and cell cycle arrest induced by 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole (5F 203, NSC 703786) is attenuated in aryl hydrocarbon receptor deficient MCF-7 cells (2003) (95)
Structural studies on bioactive compounds. 23. Synthesis of polyhydroxylated 2-phenylbenzothiazoles and a comparison of their cytotoxicities and pharmacological properties with genistein and quercetin. (1994) (94)
Antitumour benzothiazoles. Part 10: the synthesis and antitumour activity of benzothiazole substituted quinol derivatives. (2000) (92)
Benzylidene derivatives of andrographolide inhibit growth of breast and colon cancer cells in vitro by inducing G1 arrest and apoptosis (2008) (91)
Pharmacodynamics of the G-Quadruplex-Stabilizing Telomerase Inhibitor 3,11-Difluoro-6,8,13-trimethyl-8H-quino[4,3,2-kl]acridinium methosulfate (RHPS4) in Vitro: Activity in Human Tumor Cells Correlates with Telomere Length and Can Be Enhanced, or Antagonized, with Cytotoxic Agents (2005) (89)
Aryl hydrocarbon receptor mediates sensitivity of MCF-7 breast cancer cells to antitumor agent 2-(4-amino-3-methylphenyl) benzothiazole. (2002) (89)
G-Quadruplex Ligand RHPS4 Potentiates the Antitumor Activity of Camptothecins in Preclinical Models of Solid Tumors (2008) (88)
4-Substituted 4-hydroxycyclohexa-2,5-dien-1-ones with selective activities against colon and renal cancer cell lines. (2003) (85)
Metabolic activation of temozolomide measured in vivo using positron emission tomography. (2003) (85)
Preclinical evaluation of amino acid prodrugs of novel antitumor 2-(4-amino-3-methylphenyl)benzothiazoles. (2002) (85)
The discovery of the potent and selective antitumour agent 2-(4-amino-3-methylphenyl)benzothiazole (DF 203) and related compounds. (2001) (82)
In vitro, in vivo, and in silico analyses of the antitumor activity of 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazoles. (2004) (81)
Recognition and stabilization of quadruplex DNA by a potent new telomerase inhibitor: NMR studies of the 2:1 complex of a pentacyclic methylacridinium cation with d(TTAGGGT)4 (2001) (79)
Elucidation of thioredoxin as a molecular target for antitumor quinols. (2005) (75)
Antitumor polycyclic acridines. 20. Search for DNA quadruplex binding selectivity in a series of 8,13-dimethylquino[4,3,2-kl]acridinium salts: telomere-targeted agents. (2008) (74)
Structural studies on bioactive compounds. 40.(1) Synthesis and biological properties of fluoro-, methoxyl-, and amino-substituted 3-phenyl-4H-1-benzopyran-4-ones and a comparison of their antitumor activities with the activities of related 2-phenylbenzothiazoles. (2006) (69)
Antitumour polycyclic acridines. Part 5.1 Synthesis of 7H-pyrido[4,3,2-kl]acridines with exploitable functionality in the pyridine ring (1998) (69)
Selectivity of small molecule ligands for parallel and anti-parallel DNA G-quadruplex structures. (2009) (66)
Influence of 2-(4-aminophenyl)benzothiazoles on growth of human ovarian carcinoma cells in vitro and in vivo. (1998) (65)
The regiospecific synthesis of 5- and 7-monosubstituted and 5,6-disubstituted 2-arylbenzothiazoles† (2000) (63)
In vitro evaluation of amino acid prodrugs of novel antitumour 2-(4-amino-3-methylphenyl)benzothiazoles (2002) (63)
TRF2 inhibition triggers apoptosis and reduces tumourigenicity of human melanoma cells. (2006) (63)
CYP2S1 and CYP2W1 Mediate 2-(3,4-Dimethoxyphenyl)-5-Fluorobenzothiazole (GW-610, NSC 721648) Sensitivity in Breast and Colorectal Cancer Cells (2011) (63)
Synthesis, antitumor evaluation, and apoptosis-inducing activity of hydroxylated (E)-stilbenes. (2005) (62)
Antitumor imidazotetrazines. 41. Conjugation of the antitumor agents mitozolomide and temozolomide to peptides and lexitropsins bearing DNA major and minor groove-binding structural motifs. (2002) (61)
From triazines and triazenes to temozolomide. (1993) (60)
Antitumor polycyclic acridines. 7. Synthesis and biological properties of DNA affinic tetra- and pentacyclic acridines. (2000) (58)
*Semisynthesis and cytotoxic activities of andrographolide analogues (2006) (57)
Novel Thioredoxin Inhibitors Paradoxically Increase Hypoxia-Inducible Factor-α Expression but Decrease Functional Transcriptional Activity, DNA Binding, and Degradation (2006) (53)
Experimental antitumor activity against murine tumor model systems of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one (mitozolomide), a novel broad-spectrum agent. (1985) (51)
FLUORINATED 2-(4-AMINO-3-METHYLPHENYL)BENZOTHIAZOLES INDUCE CYP1A1 EXPRESSION, BECOME METABOLIZED, AND BIND TO MACROMOLECULES IN SENSITIVE HUMAN CANCER CELLS (2004) (51)
Cytotoxic and antiangiogenic activity of AW464 (NSC 706704), a novel thioredoxin inhibitor: an in vitro study (2005) (50)
Quinols as novel therapeutic agents. 2.(1) 4-(1-Arylsulfonylindol-2-yl)-4-hydroxycyclohexa-2,5-dien-1-ones and related agents as potent and selective antitumor agents. (2005) (49)
Phase I clinical trial of mitozolomide. (1985) (48)
Antitumor imidazotetrazines. 25. Crystal structure of 8-carbamoyl-3-methylimidazo[5,1-d]-1,2,3,5-tetrazin-4(3H)-one (temozolomide) and structural comparisons with the related drugs mitozolomide and DTIC. (1992) (48)
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones. (1987) (46)
Triazines and related products. Part 19. 4-Amino-2-[2-(piperid-n-1-ylazo)phenyl]quinazoline and its analogues. (1977) (45)
Structural studies on bioactive compounds. 32. Oxidation of tyrphostin protein tyrosine kinase inhibitors with hypervalent iodine reagents. (2000) (44)
Antitumor benzothiazoles. Frontier molecular orbital analysis predicts bioactivation of 2-(4-aminophenyl)benzothiazoles to reactive intermediates by cytochrome P4501A1. (2003) (42)
Antitumor polycyclic acridines. 17. Synthesis and pharmaceutical profiles of pentacyclic acridinium salts designed to destabilize telomeric integrity. (2005) (42)
The Experimental Antitumor Agents Phortress and Doxorubicin are Equiactive Against Human-Derived Breast Carcinoma Xenograft Models (2004) (40)
Quinols as novel therapeutic agents. 7.1 Synthesis of antitumor 4-[1-(arylsulfonyl-1H-indol-2-yl)]-4-hydroxycyclohexa-2,5-dien-1-ones by Sonogashira reactions. (2007) (40)
Antitumour benzothiazoles. Part 32: DNA adducts and double strand breaks correlate with activity; synthesis of 5F203 hydrogels for local delivery. (2015) (36)
The G-quadruplex-stabilising agent RHPS4 induces telomeric dysfunction and enhances radiosensitivity in glioblastoma cells. (2015) (35)
Pyrazolo-as-triazines. Part I (1966) (35)
Structural studies on bioactive compounds. Part 36: design, synthesis and biological evaluation of pyrimethamine-based antifolates against Pneumocystis carinii. (2002) (34)
Induction of apoptosis without redox catastrophe by thioredoxin-inhibitory compounds. (2003) (34)
Structural studies on bioactive compounds. 4. A structure-antitumor activity study on analogues of N-methylformamide. (1986) (34)
DNA Damage Persistence as Determinant of Tumor Sensitivity to the Combination of Topo I Inhibitors and Telomere-Targeting Agents (2011) (34)
Mechanisms of acquired resistance to 2-(4-Amino-3-methylphenyl)benzothiazole in breast cancer cell lines (2008) (33)
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents. (1990) (33)
Structure and K+ ion-dependent stability of a parallel-stranded DNA quadruplex containing a core A-tetrad. (2004) (33)
Identification of novel RHPS4-derivative ligands with improved toxicological profiles and telomere-targeting activities (2014) (32)
A new light on the photo‐decomposition of the antitumour drug DTIC (1981) (32)
Antitumor Imidazotetrazines. 35. New Synthetic Routes to the Antitumor Drug Temozolomide. (1997) (31)
Azidoacridines; potential nucleic acid mutagens. (1972) (30)
2-(4-Amino-3-methylphenyl)-5-fluorobenzothiazole is a ligand and shows species-specific partial agonism of the aryl hydrocarbon receptor. (2009) (30)
The mass spectra of s-triazines (1970) (30)
N-Methylformamide (NSC 3051): a potential candidate for combination chemotherapy. (1985) (30)
Antitumour polycyclic acridines. Palladium(0) mediated syntheses of quino[4,3,2-kl]acridines bearing peripheral substituents as potential telomere maintenance inhibitors. (2003) (29)
Antitumour polycyclic acridines. Part 1. Synthesis of7H-pyrido- and 8H-quino-[4,3,2-kl]acridinesby Graebe–Ullmann thermolysis of 9-(1,2,3-triazol-1-yl)acridines:application of differential scanning calorimetry to predict optimumcyclisation conditions (1997) (29)
Synthesis of water-soluble prodrugs of the cytotoxic agent Combretastatin A4 (1996) (28)
Antitumor imidazotetrazines. 40. Radiosyntheses of [4-11C-carbonyl]- and [3-N-11C-methyl]-8-carbamoyl-3-methylimidazo[5,1-d]-1,2,3,5-tetrazin-4(3H)-one (temozolomide) for positron emission tomography (PET) studies. (2002) (28)
Antitumour imidazotetrazines. Part 39. Synthesis of bis(imidazotetrazine)s with saturated spacer groups (2000) (28)
Antitumor Quinol PMX464 Is a Cytocidal Anti-trypanosomal Inhibitor Targeting Trypanothione Metabolism* (2011) (27)
Ligand selectivity in stabilising tandem parallel folded G-quadruplex motifs in human telomeric DNA sequences. (2014) (27)
α-hydroxylated derivatives of antitumour dimethyltriazenes (1978) (27)
Studies of the mode of action of antitumour triazenes and triazines-II. Investigation of the selective toxicity of 1-aryl-3,3-dimethyltriazenes. (1981) (27)
Decomposition of the antitumour drug temozolomide in deuteriated phosphate buffer: methyl group transfer is accompanied by deuterium exchange (1993) (26)
Certain Imidazotetrazines Escape O6-Methylguanine-DNA Methyltransferase and Mismatch Repair (2011) (26)
Antitumour benzothiazoles. Part 15: The synthesis and physico-chemical properties of 2-(4-aminophenyl)benzothiazole sulfamate salt derivatives. (2001) (26)
Antitumour imidazotetrazines. Part 36.1 Conversion of 5-aminoimidazole-4-carboxamide to imidazo[5,1-d][1,2,3,5]tetrazin-4(3H)-ones and imidazo[1,5-a][1,3,5]triazin-4(3H)-ones related in structure to the antitumour agents temozolomide and mitozolomide (1998) (25)
Structural studies on bio-active compounds. Part XIV. Molecular modelling of the interactions between pentamidine and DNA. (1990) (25)
NMR studies of multiple conformations in complexes of Lactobacillus casei dihydrofolate reductase with analogues of pyrimethamine. (1990) (25)
Structural Studies on Bioactive Compounds. Part 38.1 Reactions of 5-Aminoimidazole-4-Carboxamide: Synthesis of Imidazo[1,5-a]Quinazoline-3-Carboxamides † (2003) (25)
Oxidative metabolism of some N-methyl containing xenobiotics can lead to stable progenitors of formaldehyde. (1979) (25)
The chemosensitivity of a new experimental model--the M5076 reticulum cell sarcoma. (1984) (25)
Mechanisms of acquired resistance to 2-(4-aminophenyl)benzothiazole (CJM 126, NSC 34445) (2000) (24)
Structural studies on bio-active compounds. Part XV. Structure-activity relationships for pyrimethamine and a series of diaminopyrimidine analogues versus bacterial dihydrofolate reductase. (1989) (23)
Antitumour imidazotetrazines. Part 12. Reactions of mitozolomide and its 3-alkyl congeners with oxygen, nitrogen, halogen, and carbon nucleophiles (1987) (23)
Structure of Mycobacterium tuberculosis thioredoxin C. (2006) (22)
Antitumour benzothiazoles. Part 2. Formation of 2,2′-diaminobiphenyls from the decomposition of 2-(4-azidophenyl)benzazoles in trifluoromethanesulfonic acid (1996) (22)
The formation and metabolism of N-hydroxymethyl compounds--IV. Cytotoxicity and antitumour activity of N-hydroxymethylformamide, a putative metabolite of N-methylformamide (NSC 3051). (1983) (22)
Studies of the mode of action of antitumor triazenes and triazines. 6. 1-Aryl-3-(hydroxymethyl)-3-methyltriazenes: synthesis, chemistry, and antitumor properties. (1984) (22)
Cyclisation reactions of azolylhydrazones derived from ethyl cyanoacetate and malononitrile. Formation of azolo[5,1-c][1,2,4]triazines (1976) (22)
Fused imidazoles as potential chemical scaffolds for inhibition of heat shock protein 70 and induction of apoptosis. Synthesis and biological evaluation of phenanthro[9,10-d]imidazoles and imidazo[4,5-f][1,10]phenanthrolines. (2016) (21)
Anti-tumour imidazotetrazines. Part XXI. Mitozolomide and temozolomide: probes for the major groove of DNA. (1990) (21)
Structural studies on bio-active compounds. Part 5. Synthesis and properties of 2,4-diaminopyrimidine dihydrofolate reductase inhibitors bearing lipophilic azido groups (1987) (21)
RHPS4 G-Quadruplex Ligand Induces Anti-Proliferative Effects in Brain Tumor Cells (2014) (20)
On and off-target effects of telomere uncapping G-quadruplex selective ligands based on pentacyclic acridinium salts (2013) (20)
Antitumour polycyclic acridines. Part 3.1 A two-step conversion of 9-azidoacridine to 7H-pyrido[4,3,2-kl]acridines by Graebe–Ullmann thermolysis of substituted 9-(1,2,3-triazol-1-yl)acridines (1998) (20)
Crystal structure and molecular modelling of the antimicrobial drug pentamidine (1989) (20)
Triazines and related products. Part 23. New photo-products from 5-diazoimidazole-4-carboxamide (Diazo-IC) (1981) (20)
Synthesis and antitumour evaluation of novel 2-phenylbenzimidazoles (2008) (19)
Structural studies on bioactive compounds. 30. Crystal structure and molecular modeling studies on the Pneumocystis carinii dihydrofolate reductase cofactor complex with TAB, a highly selective antifolate. (2000) (19)
Delivery of temozolomide and N3-propargyl analog to brain tumors using an apoferritin nanocage. (2020) (18)
Carbene reactivity of 4-diazo-4H-imidazoles toward nucleophiles and aromatic compounds. (2009) (18)
ANTITUMOUR IMIDAZOTETRAZINES. 1. SYNTHESIS AND CHEMISTRY OF 8-CARBAMOYL-3-(2-CHLOROETHYL)IMIDAZO(5,1-D)-1,2,3,5-TETRAZIN-4(3H)-ONE, A NOVEL BROAD-SPECTRUM ANTITUMOR AGENT (1984) (18)
Role of CYP 1 A 1 in Modulation of Antitumor Properties of the Novel Agent 2-( 4-Amino-3-methylphenyl ) benzothiazole ( DF 203 , NSC 674495 ) in Human Breast Cancer Cells 1 (2000) (18)
Preclinical Toxicokinetic Evaluation of Phortress [2-(4-Amino-3-Methylphenyl)-5-Fluorobenzothiazole Lysylamide Dihydrochloride] in Two Rodent Species (2008) (18)
Structural studies on bioactive compounds. Part 29: palladium catalysed arylations and alkynylations of sterically hindered immunomodulatory 2-amino-5-halo-4,6-(disubstituted)pyrimidines. (2000) (18)
Antitumor polycyclic acridines. Part 12. Physical and biological properties of 8,13-diethyl-6-methylquino[4,3,2-kl]acridinium iodide: a lead compound in anticancer drug design. (2002) (18)
Antitumor quinols: role of glutathione in modulating quinol-induced apoptosis and identification of putative cellular protein targets. (2006) (17)
Quinol derivatives as potential trypanocidal agents (2012) (17)
Structural studies on bioactive compounds. 34. Design, synthesis, and biological evaluation of triazenyl-substituted pyrimethamine inhibitors of Pneumocystis carinii dihydrofolate reductase. (2001) (17)
N3-Substituted Temozolomide Analogs Overcome Methylguanine-DNA Methyltransferase and Mismatch Repair Precipitating Apoptotic and Autophagic Cancer Cell Death (2014) (16)
Antitumour polycyclic acridines. Part 4. Physico-chemical studies on the interactions between DNA and novel tetracyclic acridine derivatives. (1998) (15)
The mass spectra of 1,2,4‐triazines and related compounds (1971) (15)
Studies of the mode of action of antitumour triazenes and triazines--IV. The metabolism of 1-(4-acetylphenyl)-3,3-dimethyltriazene. (1982) (15)
Molecular recognition between a new pentacyclic acridinium salt and DNA sequences investigated by optical spectroscopic techniques, proton nuclear magnetic resonance spectroscopy, and molecular modeling. (1999) (15)
A 15N NMR investigation of a series of benzotriazinones and related antitumour heterocycles (2002) (15)
Antitumour polycyclic acridines. Part 10. Synthesis of penta- and hexa-cyclic heteroaromatic systems by radical cyclisations of substituted 9-anilinoacridines (2001) (14)
Structure of Mycobacterium tuberculosis thioredoxin in complex with quinol inhibitor PMX464 (2011) (14)
Triazines and related products. Part 26. Synthesis and chemistry of bicyclic analogues of the antitumour drug 2,4,6-tris(dimethylamino)-1,3,5-triazine (hexamethylmelamine) (1984) (14)
Structural studies on bioactive compounds. 8. Synthesis, crystal structure, and biological properties of a new series of 2,4-diamino-5-aryl-6-ethylpyrimidine dihydrofolate reductase inhibitors with in vivo activity against a methotrexate-resistant tumor cell line. (1989) (14)
Antitumour imidazotetrazines. Part 31. The synthesis of isotopically labelled temozolomide and a multinuclear (1H, 13C, 15N) magnetic resonance investigation of temozolomide and mitozolomide (1995) (14)
Studies of the mode of action of antitumour triazenes and triazines-V. The correlation of the in vitro cytotoxicity and in vivo antitumour activity of hexamethylmelamine analogues with their metabolism. (1984) (14)
Methyl p-coumarate: A cytotoxic constituent from Comptonia peregrina (1984) (14)
C8-Substituted Imidazotetrazine Analogs Overcome Temozolomide Resistance by Inducing DNA Adducts and DNA Damage (2019) (13)
708. Cyclic amidines. Part XVII. 4-Imino-1,2,3-benzotriazines (1964) (13)
Triazines and related products. Part X. A re-examination of the reaction between benzil and diaminoguanidine nitrate (1972) (13)
Structural studies on bioactive compounds. 28. Selective activity of triazenyl-substituted pyrimethamine derivatives against Pneumocystis carinii dihydrofolate reductase. (1997) (13)
Triazines and related products. Part 18. Decomposition of 1,2,3-benzotriazines and related triazenes with sodium azide in acetic acid: a convenient route to azidoarenes (1977) (13)
SYNTHETIC STUDIES OF 8-CARBAMOYLIMIDAZO-5,1-D-1,2,3,5-TETRAZIN-4(3H)-ONE :A KEY DERIVATIVE OF ANTITUMOUR DRUG TEMOZOLOMIDE (1996) (13)
Antitumor Benzothiazoles. Part 20. 3′-Cyano and 3′-Alkynyl-Substituted 2-(4′-Aminophenyl)benzothiazoles as New Potent and Selective Analogues. (2003) (13)
Synthetic strategies to a telomere-targeted pentacyclic heteroaromatic salt. (2007) (12)
Triazines and related products. Part XV. 2,4-Diaminopyrimidines and 2-aminopyrimidin-4(3H)-ones bearing 1,2,3-benzotriazinyl groups as potential dihydrofolic reductase inhibitors. (1975) (12)
Studies on the toxicity of the antitumour agent N-methylformamide in mice. (1985) (12)
Brampton, M, Stevens MFG. Cancer Research Campaign phase-II trial of temozolomide in malignant melanoma (1995) (12)
Triazines and related products. Part 21. Cyclisation of 3-amino-5-hydrazinopyrazole and 3-amino-5-hydrazino-1,2,4-triazole to azolo[5,1-c][1,2,4]triazines (1978) (12)
A concise synthesis of either enantiomer of azatyrosine (1996) (11)
Antitumour imidazotetrazines. Part 33. New syntheses of the antitumour drug temozolomide using ‘masked’ methyl isocyanates (1995) (11)
Synthesis and properties of bioactive 2- and 3-amino-8-methyl-8H-quino[4,3,2-kl]acridine and 8,13-dimethyl-8H-quino[4,3,2-kl]acridinium salts. (2004) (10)
Antitumour Polycyclic Acridines. Part 13.1 Synthesis of 2-Substituted 7H-Pyrido[4,3,2-kl]Acridines by Thermolysis of 9-(5-Alkyltriazol-1-yl)Acridines † (2003) (10)
Triazines and related products, Part 22. Synthesis and reactions of imidazo[5,1-c][1,2,4]triazines (1981) (10)
Selective Reactions in the Triazene Series; I. Reduction of 1-(4-Acetylphenyl)-triazenes (1983) (10)
Triazines and related products. Part 25. Methods for the attachment of sugar residues to cytotoxic 1,3,5-triazines (1982) (10)
Formulation Studies on [2-amino-5-bromo-phenyl-4(3)-pyrimidinone] (ABPP), an Interferon Inducer. Anti-Cancerogenic Agent (1986) (10)
The aromatic azido group in anti-cancer drug design: application in the development of novel lipophilic dihydrofolate reductase inhibitors. (1987) (10)
Hitting the chemotherapy jackpot: strategy, productivity and chemistry. (2004) (10)
A New Synthesis of Aminoquinazolines (1969) (10)
Triazines and related products. Part III. Synthesis and rearrangement of 3,4-dihydro-4-imino-1,2,3-benzotriazines (1970) (10)
Synthesis of 6-arylisocytosines and their potential for hydrogen bonding interactions (2015) (9)
Triazines and related products. Part 24. Synthesis of pyrazol-4-ylidenehydrazinoimidazoles by hydrazinolysis of imidazo[5,1-c][1,2,4]-triazines and 2-arylazoimidazoles by diazonium coupling reactions (1982) (9)
Synthesis of antitumour (1H-1,2,3-triazol-4-yl)-4-hydroxycyclohexa-2,5-dien-1-ones by copper-catalysed Huisgen cycloadditions. (2010) (9)
STRUCTURAL STUDIES ON BIO-ACTIVE COMPOUNDS. PART 2. THE SOLID-STATE AND SOLUTION CONFORMATIONS OF N-METHYL-2-NITROETHENAMINE AND RELATED COMPOUNDS (1985) (9)
In search of effective therapies to overcome resistance to Temozolomide in brain tumours (2019) (9)
Introduction of a triflate group into sterically-hindered positions in 1-aryl-4,6-diamino-1,3,5-triazines and their Dimroth rearrangement products (1993) (9)
Triazines and related products. Part I. 1,3-di-O-cyanophenyltriazene (1967) (9)
Alternative syntheses of the antitumlur drug temozolomide avoiding the use of methyl isocyanate (1994) (9)
Antitumor imidazotetrazines. 38. New 8-substituted derivatives of the imidazo[5,1-d]-1,2,3,5-tetrazines temozolomide and mitozolomide (2000) (9)
Antitumor polycyclic acridines. Part 16. Triplex DNA as a target for DNA-binding polycyclic acridine derivatives. (2005) (9)
Pyrazolotriazines: a new class of tumour‐inhibitory agents (1966) (8)
A Revised Synthesis of the Antitumour Antibiotic L-azatyrosine via 2-iodo-5-methoxypyridine (2001) (8)
Antitumour imidazotetrazines. Synthesis and chemistry of 4-oxo-3,4-dihydroimidazo[5,1-d][1,2,3,5]tetrazine-8-carboxamide (nor-temozolomide): an intermediate for the preparation of the antitumour drug temozolomide and analogues, avoiding the use of isocyanates (2012) (8)
A new route to the antitumour drug temozolomide, but not thiotemozolomide (1997) (8)
Triazines and related products. Part VIII. Potential irreversible chymotrypsin inhibitors: 3-Alkyl-1,2,3-benzotriazin-4(3H)-ones and o-azidobenzamides (1971) (8)
Antitumour activity, biomimetic oxidation and metabolism of heteroalicyclic triazenes. (1979) (8)
Antitumor benzothiazoles. 13. (Diacetoxy)iodobenzene (DAIB) oxidation of 2-(4-hydroxy-3-methoxyphenyl)benzothiazole and related compounds in the presence of dienophiles (2000) (8)
Novel reaction products from the hypervalent iodine oxidation of hydroxylated stilbenes and isoflavones. (2005) (8)
Temozolomide: From Cytotoxic to Molecularly Targeted Agent (2008) (8)
Structural studies on bioactive compounds. 39. Biological consequences of the structural modification of DHFR-inhibitory 2,4-diamino-6-(4-substituted benzylamino-3-nitrophenyl)-6-ethylpyrimidines ('benzoprims'). (2004) (8)
Structural studies on bioactive compounds. Part 26. Hydrogen bonding in the crystal structure of the N-methylformamide solvate of the immunomodulatory agent 2-amino-5-bromo-6-phenylpyrimidin-4-one (bropirimine): implications for the design of novel anti-tumour strategies. (1995) (7)
Structural studies on bio-active compounds. Part 3. Re-examination of the hydrolysis of the antimalarial drug pyrimethamine and related derivatives and crystal structure of a hydrolysis product (1985) (7)
Triazines and related products. Part XVI. Synthesis of triazolotriazines by cyclisation of 3-hydrazino-1,2,4-triazines and 3-hydrazino-1,2,4-triazoles (1976) (7)
Triazines and related products. Part V. The structure of some red N-alkyl-1,2,3-benzotriazines (1970) (7)
Structural studies on bio-active compounds. 20. Molecular modeling and crystallographic studies on methylbenzoprim, a potent inhibitor of dihydrofolate reductase. (1992) (7)
Antitumour polycyclic acridines. Part 9. Synthesis of 7H-pyrido[4,3,2-kl]acridines with basic side chains (2001) (7)
Antitumor Polycyclic Acridines. Part 7. Synthesis and Biological Properties of DNA Affinic Tetra- and Pentacyclic Acridines. (2000) (7)
Structural studies on bio-active compounds. Part 6. Determination of the sites of protonation on three 2,4-diaminopyrimidines of pharmaceutical importance by proton-coupled 13C and 1H nuclear magnetic resonance spectroscopy (1987) (7)
Decomposition of 2-(4-azidophenyl)benzothiazoles in trifluoromethanesulfonic acid: formation of 2,2′-diaminobiphenyls (1992) (6)
The antitumour activity of 2‐(4‐amino‐3‐methylphenyl)‐5‐fluorobenzothiazole in human gastric cancer models is mediated by AhR signalling (2019) (6)
Antitumor Benzothiazoles. Part 10. The Synthesis and Antitumor Activity of Benzothiazole Substituted Quinol Derivatives. (2000) (6)
Aminomethinylation of aromatic amines (1969) (6)
Triazines and related products. Part 28. Conversion of 3-aryl-1-(2-cyanophenyl)triazenes into 3-arylquinazolin-4(3H)-ones with formamide (1985) (6)
Chemosensitization of Temozolomide-Resistant Pediatric Diffuse Midline Glioma Using Potent Nanoencapsulated Forms of a N(3)-Propargyl Analogue. (2021) (6)
Experimental Background and Early Clinical Studies with Imidazotetrazine Derivatives (1990) (6)
Antitumour imidazotetrazines, Part IX. The pharmacokinetics of mitozolomide in mice. (1985) (6)
Antitumor Imidazotetrazines. Part 12. Reactions of Mitozolomide and Its 3-Alkyl Congeners with Oxygen, Nitrogen, Halogen, and Carbon Nucleophiles. (1987) (6)
Antitumor imidazo[5,1-d]-1,2,3,5-tetrazines: compounds modified at the 3-position overcome resistance in human glioblastoma cell lines (2016) (6)
Triazines and related products. Part XIII. Decomposition of 4-Arylamino-1,2,3-benzotriazines and their precursors in secondary amines (1974) (6)
Pyrazolo-as-triazines. Part III. Ring fission (1967) (6)
Antitumour imidazotetrazines. Part 5. Crystal and molecular structure of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3h)-one (mitozolomide) (1985) (6)
Structural Studies on Bioactive Compounds. Part 37.1 Suzuki Coupling of Diaminopyrimidines: A New Synthesis of the Antimalarial Drug Pyrimethamine † (2002) (6)
Antitumor Polycyclic Acridines. Part 5. Synthesis of 7H‐Pyrido[4,3,2‐kl]acridines with Exploitable Functionality in the Pyridine Ring. (1998) (5)
Confirmation of the site of nitrosation in tryptophan derivatives by α-chymotrypsin (1975) (5)
Abstract B59: Preliminary clinical experiences of Phortress: Putative role for c‐MET inhibition in antitumor activity (2009) (5)
Antitumour benzothiazoles. Part 4. An NMR study of the sites of protonation of 2-(4-aminophenyl)benzothiazoles (1996) (5)
Triazines and related products. Part XII. Reactions of 3,4-dihydro-4-imino-1,2,3-benzotriazines and 1,2,3-benzotriazin-4(3H)-ones in secondary amines (1974) (5)
THE ANALYSIS AND MURINE PHARMACOKINETICS OF A NEW ANTITUMOUR AGENT: CCRG81045 (1986) (5)
Triazines and related products. Part XIV. Decomposition of 1,2,3-benzotriazin-4(3H)-ones in the presence of reactive methylene systems (1974) (5)
Quinols as novel therapeutic agents. 8. Applications of the Sonogashira route to thioredoxin-inhibitory indolyl-substituted quinols (2007) (4)
Relationship between the pharmacokinetics and toxicity of mitozolomide (2004) (4)
Anthraniloylanthranilamide (o-amino-N-(o-carbamoylphenyl)benzamide): Preparation and use as a synthetic precursor for quinazolino[1,2,3]benzotriazinones (1978) (4)
441 POSTER The G-quadruplex ligand RHPS4 potentiates the antitumor activity of camptothecins in preclinical models of solid tumors (2008) (4)
Triazines and related products. IX. Potential irreversible dihydrofolate reductase inhibitors: 2,4-diamino-S-triazines with a masked covalent labelling group. (1972) (4)
Synthesis and antitumour evaluation of novel 2-phenylbenzimidazoles. (2008) (4)
Pyrazolo-as-triazines. Part II. Bromination (1966) (4)
6,7-Diphenyl[1,2,4]triazolo[5,1-c][l,2,4]triazine (1978) (4)
Metabolism and murine pharmacokinetics of the 8-(N,N-dimethylcarboxamide) analogue of the experimental antitumor drug mitozolomide (NSC353451). (1989) (4)
479 POSTER Acquired resistance to temozolomide in glioma cell lines: molecular mechanisms and potential translational applications (2008) (4)
Triazines and related products. Part 30. Cationic analogues of the antitumour drug 2,4,6-tris(dimethylamino)-1,3,5-triazine (hexamethylmelamine) (1985) (4)
Triazines and related products. Part XI. Dimroth rearrangements of 3-substituted 3,4-dihydro-4-imino-1,2,3-benzotriazines in acetic acid (1974) (4)
Triazines and related products. Part VII. Reductive fission of 1,2,3-benzotriazines with hydrazine and Raney nickel (1970) (4)
Triazines and related products. Part VI. Synthesis and properties of 4-amino-2(2H)-imino-s-triazino[1,2-c][1,2,3]-benzotriazines (1970) (4)
Mass spectra of diaryltriazenes and 1,2,3-benzotriazines (1970) (4)
Triazines and related products. Part IV. Methylation of 3-aryl-3,4-dihydro-4-imino-1,2,3-benzotriazines (1970) (4)
Reassignment of the stereochemistry of oblonginine (1998) (4)
Ring-expansion of azidobenzenesulphonamides and azidobenzamides (1983) (4)
Erratum: Identification of novel RHPS4-derivative ligands with improved toxicological profiles and telomere-targeting activities (2015) (4)
Antitubercular Properties of Substituted Hydroxycyclohexadienones (2006) (4)
Structural Studies on Bioactive Compounds. Part 31. Interaction of 9-azidoacridine and 1-morpholinocyclohexene: Formation, Decomposition and Rearrangement of the Intermediate 1,2,3-triazoline † (2000) (3)
NMR and Molecular Modelling Studies on the Mechanism of Action of the Antitumour Drug Temozolomide (1995) (3)
Triazines and related products. Part 27. Thermolysis of 4-anilino-1,2,3-benzotriazines (1984) (3)
Biological Activity of the G-quadruplex Ligand RHPS4 is Associated with Telomere Capping Alteration (2004) (3)
Synthesis and growth-inhibitory activities of imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamides related to the anti-tumour drug temozolomide, with appended silicon, benzyl and heteromethyl groups at the 3-position. (2018) (3)
2-(4-Aminophenyl)benzothiazoles: Agents with Selective and Potent Antitumour Activity in vitro and in vivo (1999) (3)
Structural studies on bioactive compounds. 1 Heck reactions on 4-methylenepyrazolo[5,1-c][1,2,4]triazines (2008) (3)
Antitumor Benzothiazoles. Part 14. Synthesis and in vitro Biological Properties of Fluorinated 2-(4-Aminophenyl)benzothiazoles. (2010) (3)
Structural studies on bio-active compounds. Part 9. 2,4-Diamino-6-azidoquinazoline hydrochloride. (1987) (3)
Triazines and related products. Part 20. Oxidation of 1-(arylazo)-piperidines with potassium permanganate. (1977) (3)
Medicinal nitro-compounds. Part II. Search for ortho-interactions in tumour-inhibitory 2,4-dinitrophenylaziridines. (1975) (3)
DTIC: A Springboard to New Antitumour Agents (1983) (3)
Structural studies on bioactive compounds. Part 33. ‡ Synthesis of 9-arylacridines by palladium-mediated couplings † (2000) (3)
Antitumor Imidazotetrazines. Part 39. Synthesis of Bis(imidazotetrazine)s with Saturated Spacer Groups. (2001) (3)
Temozolomide analog PMX 465 downregulates MGMT expression in HCT116 colorectal carcinoma cells (2018) (3)
Medicinal nitro-compounds. Part I. Photo-rearrangement of N-aryl-2-nitrobenzamides (1973) (2)
Pharmacodynamics of the G-quadruplex-stabilizing telomerase inhibitor RHPS 4 in vitro : activity in human tumor cells correlates with telomere length and can be enhanced , or antagonized , with cytotoxic agents (2005) (2)
Antitumor Benzothiazoles. Part 15. The Synthesis and Physico‐Chemical Properties of 2‐(4‐Aminophenyl)benzothiazole Sulfamate Salt Derivatives. (2001) (2)
TRIAZINES AND RELATED PRODUCTS. PART 24. SYNTHESIS OF PYRAZOL-4-YLIDENEHYDRAZINOIMIDAZOLES BY HYDRAZINOLYSIS OF IMIDAZO(5,1-C)(1,2,4)TRIAZINES AND 2-ARYLAZOIMIDAZOLES BY DIAZONIUM COUPLING REACTIONS (1982) (2)
Reaction of 3-methylindole with a diazonium salt (1975) (2)
Structural studies on bioactive compounds. Part 27. Chemistry of the immunomodulatory agent bropirimine. (1995) (2)
STUDIES OF THE MODE OF ACTION OF ANTITUMOR TRIAZENES AND TRIAZINES. 6. 1-ARYL-3-(HYDROXYMETHYL)-3-METHYLTRIAZENES: SYNTHESIS, CHEMISTRY, AND ANTITUMOR PROPERTIES (1984) (2)
430 POSTER Telomere Damage promotes antitumoral activity of the G-quadruplex ligand RHPS4 (2006) (2)
Antitumor Imidazotetrazines. Part 14. Synthesis and Antitumor Activity of 6‐ and 8‐Substituted Imidazo(5,1‐d)‐1,2,3,5‐tetrazinones and 8‐Substituted Pyrazolo(5,1‐d)‐1,2,3,5‐tetrazinones. (1987) (2)
Is there a future for the small molecule in developmental cancer chemotherapy (1992) (2)
Antitumour polycyclic acridines. Part 2. Physicochemical studies on the interactions between DNA and novel polycyclic acridine derivatives. (1998) (2)
Gene Expression Profiling of 2-(4-Aminophenyl)benzothiazole-resistant MCF-7 Cells Using cDNA Microarrays. (2004) (2)
Triazines and related products. IXXX: Chemistry DHFR-inhibitory activity and antitumour activity of substituted 2,4-diamino-6-phenyl-1,3,5-triazines (1984) (2)
Radiolabelling of the potential anti‐cancer agent, 5‐fluoro‐2‐(4‐amino‐3‐methylphenyl)benzothiazole (5F203) with fluorine‐18 (2001) (2)
Synthesis of 6‐Arylisocytosines and Their Potential for Hydrogen Bonding Interactions. (2016) (2)
ANTITUMOR IMIDAZOTETRAZINES. PART 5. CRYSTAL AND MOLECULAR STRUCTURE OF 8-CARBAMOYL-3-(2-CHLOROETHYL)IMIDAZO(5,1-D)-1,2,3,5-TETRAZIN-4(3H)-ONE (MITOZOLOMIDE) (1985) (2)
Structural studies on bio-active compounds. Part 25. Synthesis and properties of potential metabolites of the diaminopyrimidine antifolate 2,4-diamino-5-(3-azido-4-chlorophenyl)-6-ethylpyrimidine (MZPES) (1994) (2)
TRIAZINES AND RELATED PRODUCTS. PART 22. SYNTHESIS AND REACTIONS OF IMIDAZO(5,1-C)(1,2,4)TRIAZINES (1981) (2)
Structural Studies on Bioactive Compounds. Part 37. Suzuki Coupling of Diaminopyrimidines: A New Synthesis of the Antimalarial Drug Pyrimethamine. (2003) (2)
Chapter 5 – Temozolomide: From Cytotoxic to Molecularly Targeted Agent (2014) (2)
Abstract A143: Novel temozolomide analog may overcome MGMT and MMR (2009) (2)
The analysis and pharmacokinetics of ccrg 81010 (m & b 39565, nsc 353451) - a new antitumor compound. Abstr. (1983) (2)
Antitumour imidazotetrazines. Part 37. Conjugation of the DNA major-groove alkylating imidazotetrazine mitozolomide to peptide motifs recognizing the minor groove. (1999) (2)
Photo-rearrangement of o-nitrobenzanilide (1972) (2)
Induction of G1 arrest and apoptosis by new benzylidene derivatives of andrographolide in breast and colon cancer cells (2007) (1)
A phase I study of meta-azidopyrimethamine ethanesulphonate (MZPES) — a new dihydrofolate reductase inhibitor (2004) (1)
Structural studies on bio-active compounds. Part 16. Synthesis and properties of sterically-constrained analogues of methylbenzoprim, a new dihydrofolate reductase inhibitor. (1990) (1)
RING EXPANSION OF AZIDOBENZENESULFONAMIDES AND AZIDOBENZAMIDES (1984) (1)
Structural Studies on Bioactive Compounds. Part 33. Synthesis of 9-Arylacridines by Palladium-Mediated Couplings. (2001) (1)
Crystal structure of anhydro‐2‐methyl‐4‐o‐nitroanilino‐1,2,3‐benzotriazinium hydroxide (1978) (1)
l-Azatyrosine: a new lead in anticancer drug development (1996) (1)
323 POSTER In vitro evaluation of potential thioredoxin inhibitors in breast cancer and endothelial cells (2006) (1)
A comparative study of the anti-tumour activity of N-methylformamide and related compounds. (1981) (1)
Antitumor Imidazotetrazines. Part 35. New Synthetic Routes to the Antitumor Drug Temozolomide. (1998) (1)
Antitumor Polycyclic Acridines. Part 13. Synthesis of 2‐Substituted 7H‐Pyrido[4,3,2‐kl]acridines by Thermolysis of 9‐(5‐Alkyltriazol‐1‐yl)acridines. (2003) (1)
On and off-target effects of telomere uncapping G-quadruplex selective ligands based on pentacyclic acridinium salts (2013) (1)
Semisynthesis and cytotoxic activities of andrographolide analogues (2006) (1)
Preclinical Development CYP 2 S 1 and CYP 2 W 1 Mediate 2-( 3 , 4-Dimethoxyphenyl )-5-Fluorobenzothiazole ( GW-610 , NSC 721648 ) Sensitivity in Breast and Colorectal Cancer Cells (2011) (1)
NovelThioredoxin Inhibitors Paradoxically Increase Hypoxia-Inducible Factor-A Expression but Decrease Functional Transcriptional Activity , DNABinding , and Degradation (2006) (1)
Antitumor Benzothiazoles. Part 3. Synthesis of 2‐(4‐Aminophenyl) benzothiazoles and Evaluation of Their Activities Against Breast Cancer Cell Lines in vitro and in vivo. (1996) (1)
Synthesis of heteroaromatic quinols, novel agents with selective activity clustered in colon and renal cell lines (2002) (1)
Antitumor Imidazotetrazines. Part 33. New Syntheses of the Antitumor Drug Temozolomide Using “Masked” Methyl Isocyanates. (1996) (1)
Chemical and Biological Properties and Mode of Action of 8-Carbamoyl-3-(2-Chloroethyl)Imidazo [5,1-d]-1,2,3,5-Tetrazin-4(3H)-One, A Novel Broad Spectrum Antitumour Agent (1984) (1)
Structure of 2,4,6‐tris(N,N‐dimethylamino)‐1,3,5‐oxadiazinium chloride dihydrate, C9H18N5O+.Cl−.2H2O (1983) (1)
176 N3-Substituted temozolomide analogs overcome methylguanine DNA methyltransferase and mismatch repair (2010) (1)
AntÂ¡tumor Activity and Pharmacokinetics in Mice of 8-Carbamoyl-3-methyl- imidazo[5,l-on-l,2,3,5-tetrazin-4(37/)-one (CCRG 81045; M & B 39831), a Novel Drug with Potential as an Alternative to Dacarbazine1 (2006) (1)
Investigations on the biological properties of the lipophilic DHFR-inhibitory benzoprims reveal non-folate modes of action and opportunities for anti-cancer drug design. (2001) (1)
Antitumor Imidazotetrazinones: Prodrugs Targeted to the Major Groove of DNA (1991) (1)
Antitumor Imidazotetrazines. Part 36. Conversion of 5‐Aminoimidazole‐4‐carboxamide to Imidazo[5,1‐d][1,2,3,5]tetrazin‐4(3H)‐ones and Imidazo[1,5‐a][1,3,5]triazin‐4(3H)‐ones Related in Structure to the Antitumor Agents Temozolomide and Mitozolomide. (1998) (1)
Composes de benzazole a usage therapeutique (1994) (0)
Abstract C170: Inhibition of poly(ADP‐ribose) polymerase (PARP) increases the therapeutic efficacy of the G‐quadruplex ligand RHPS4/irinotecan combination in cancer xenografts (2009) (0)
Erratum: Identification of novel RHPS4-derivative ligands with improved toxicological profiles and telomere-targeting activities (2015) (0)
Temozolomide: Patents and the Perils of Invention (2014) (0)
NMR structure of the parallel-stranded DNA quadruplex d(TTAGGGT)4 complexed with the telomerase inhibitor RHPS4 (2003) (0)
RHPS4 telomere-interactive molecule: an active antitumoral agent with a high therapeutic index and a favorable integration with camptothecin in preclinical models of solid tumors (2007) (0)
The Telomerase Inhibitor RHPS4 Induces Telomere Shortening, DNA-Damage and Cell Death in AML Cells and Chemosensitises Cells to Daunorubicin. (2009) (0)
Abstract C171: On‐ and off‐target effects of telomere uncapping G‐quadruplex ligands based on pentacyclic acridinium salts (2009) (0)
156 DNA damage induced by camptothecins is stabilized by G-quadruplex ligands (2010) (0)
624 POSTER Rapid induction of telomeric DNA damage response and reduction of clonogenic tumor cell growth by the telomere targeting agent RHPS4 (2006) (0)
Inhibition of poly(ADP-ribose) polymerase (PARP) increases the therapeutic efficacy of the G-quadruplex ligand RHPS4/irinotecan combination in colon cancer xenografts (2009) (0)
The G-quadruplex ligand RHPS4 interferes with telomere replication leading to ATR-dependent DNA damage response (2008) (0)
625 POSTER Progress in the preclinical development of RHPS4, a telomere signalling targeted agent (2006) (0)
Selective inhibitors of Pneumocystis carinii dihydrofolate reductase via structure-based design (2000) (0)
538 POSTER Targeting the thioredoxin system in breast cancer treatment (2006) (0)
British society for matrix biology autumn meeting (2005) (0)
Identification of novel RHPS4-derivative ligands with improved toxicological profiles and telomere-targeting activities (2014) (0)
2045 POSTER The thioredoxin system is of interest in conservative breast cancer treatment (2007) (0)
TRIAZINES AND RELATED PRODUCTS PART 12, REACTIONS OF 3,4-DIHYDRO-4-IMINO-1,2,3-BENZOTRIAZINES AND 1,2,3-BENZOTRIAZIN-4(3H)-ONES IN SECONDARY AMINES (1974) (0)
Structure and molecular modeling of the anti-infective drug pentamidine (1989) (0)
Chemical oxidation and in vitro metabolism of 1-(4-chlorophenylazo) piperidine and its heteroalicyclic analogues [proceeding]. (1976) (0)
123 Chemical and structural studies on thioredoxin-inhibitory antitumour quinols (2004) (0)
TRIAZINES AND RELATED PRODUCTS. PART 18. DECOMPOSITION OF 1,2,3-BENZOTRIAZINES AND RELATED TRIAZENES WITH SODIUM AZIDE IN ACETIC ACID- A CONVENIENT ROUTE TO AZIDOARENES (1977) (0)
alpha-Hydroxylated triazenes: potential active metabolites of anti-tumour dimethyltriazenes [proceedings]. (1978) (0)
TRIAZINES AND RELATED PRODUCTS PART 14, DECOMPOSITION OF 1,2,3-BENZOTRIAZIN-4(3H)-ONES IN THE PRESENCE OF REACTIVE METHYLENE SYSTEMS (1975) (0)
Abstract B164: Role of endoplasmic reticulum stress in mechanism of action of antitumor quinols (2009) (0)
431 POSTER Elucidation of additional targets of the thioredoxin inhibitor PMX 464 (2006) (0)
TRIAZINES AND RELATED PRODUCTS PART 13, DECOMPOSITION OF 4-ARYLAMINO-1,2,3-BENZOTRIAZINES AND THEIR PRECURSORS IN SECONDARY AMINES (1974) (0)
ANTITUMOUR IMIDAZOTETRAZINES. XXXIII: NEW SYNTHESES OF THE ANTITUMOUR DRUGTEMOZOLOMIDE USING 'MASKED' METHYL ISOCYANATES (1995) (0)
Structural Studies on Bioactive Compounds. Part 31. Interaction of 9‐Azidoacridine and 1‐Morpholinocyclohexene: Formation, Decomposition, and Rearrangement of the Intermediate 1,2,3‐Triazoline. (2000) (0)
Alternative Syntheses of the Antitumor Drug Temozolomide Avoiding the Use of Methyl Isocyanate. (1994) (0)
A Concise Synthesis of Either Enantiomer of Azatyrosine. (1997) (0)
Antitumor Polycyclic Acridines. Part 3. A Two-Step Conversion of 9-Azidoacridine to 7H-Pyrido[4,3,2-kl]acridines by Graebe—Ullmann Thermolysis of Substituted 9-(1,2,3-Triazol-1-yl)acridines. (1998) (0)
Novel lead antitumour structures from oxygenated and hydroxylated bicyclic heterocycles (2002) (0)
Azido-Substituted Antifolate Drugs: Synthesis, Structure, and Activity (1986) (0)
Preparations pharmaceutiques utilisees en therapie antitumorale (1983) (0)
Carbohydrate linked melamine derivatives (1981) (0)
Structural Studies on Bioactive Compounds. Part 23. Synthesis of Polyhydroxylated 2-Phenylbenzothiazoles and a Comparison of Their Cytotoxicities and Pharmacological Properties with Genistein and Quercetin. (2010) (0)
Process for the preparation of (3 H) -imidazo (5,1-d) -1,2,3,5-tetrazine-4-one derivatives (1982) (0)
Triplex DNA, a novel target for a structure selective DNA binding class of antitumour compounds (2001) (0)
C8-Substituted Temozolomide Analogs Overcome O6-Methylguanine-DNA Methyltransferase and Mismatch RepairPrecipitating Apoptotic Cancer Cell Death (2017) (0)
Synthesis of Water‐Soluble Prodrugs of the Cytotoxic Agent Combretastatin A4. (1996) (0)
Modulation of the acidity of the 8-carboxamide group in the temozolomide family of antitumor imidazo[5,1-d][1,2,3,5]tetrazines (2020) (0)
STRUCTURAL STUDIES ON BIO‐ACTIVE COMPOUNDS. PART 2. THE SOLID‐STATE AND SOLUTION CONFORMATIONS OF N‐METHYL‐2‐NITROETHENAMINE AND RELATED COMPOUNDS (1985) (0)
TRIAZINES AND RELATED PRODUCTS. PART 21. CYCLIZATION OF 3-AMINO-5-HYDRAZINOPYRAZOLE AND 3-AMINO-5-HYDRAZINO-1,2,4-TRIAZOLE TO AZOLO(5,1-C)(1,2,4)TRIAZINES (1978) (0)
Antitumor Polycyclic Acridines. Part 9. Synthesis of 7H-Pyrido[4,3,2-kl]acridines with Basic Side Chains. (2002) (0)
Inhibiting Topoisomerases: The Chemical and Biological Activity of Novel Pentacyclic Acridinium Salts (2001) (0)
Structural Studies on Bioactive Compounds. Part 41. Heck Reactions on 4-Methylenepyrazolo[5,1-c][1,2,4]triazines (VI). (2008) (0)
In vitro biotransformation of carbinolamine metabolites of cytotoxic dimethyltriazenes [proceedings]. (1979) (0)
MEDICINAL NITRO-COMPOUNDS PART 1, PHOTO-REARRANGEMENT OF N-ARYL-2-NITROBENZAMIDES (1973) (0)
Tetraszinderivater, their preparation and use (1983) (0)
Triazines and related products. 8. Potential irreversible chymotrypsin inhibitors: 3-alkyl-1,2,3-benzotriazin-4(3H)-ones and 0-azidobenzamides. (1971) (0)
CONDENSED BENZIMIDAZOLES OF THE TYPE 6-5-7 (1981) (0)
PC39 ANTI-ANGIOGENIC EFFECTS OF AW464, A NOVEL CHEMOTHERAPEUTIC DRUG TARGETING THIOREDOXIN-1 (2004) (0)
Correlation of the antitumour activity of hexamethylmelamine analogues with their in vitro cytotoxicity and metabolism (1982) (0)
The use of the COMPARE algorithm to guide mechanistic studies on novel antitumor agents: A tale of two benzothiazoles (2002) (0)
Summary of Poster-Sessions (1990) (0)
Influence of steric crowding on hydrogen bonding in anti-cancer quinols (2014) (0)
TRIAZINES AND RELATED PRODUCTS PART 15, 2,4-DIAMINOPYRIMIDINES AND 2-AMINOPYRIMIDIN-4(3H)-ONES BEARING 1,2,3-BENZOTRIAZINYL GROUPS AS POTENTIAL DIHYDROFOLIC REDUCTASE INHIBITORS (1975) (0)
Condensed Benzimidazoles of Type 6‐5‐7 and Higher Homologs (2008) (0)
3H-imidazo-5,1-d-1,2,3,5-tetrazine-4-one derivatives processes for their preparation and pharmaceutical compositions containing them (1982) (0)
The biological and chemical properties of 4-azidobenzenesulphonamide ('azidosulphanilamide') [proceedings]. (1979) (0)
Synthetic Studies of 8‐Carbamoylimidazo‐(5,1‐d)‐1,2,3,5‐tetrazin‐4(3H)‐ one: A Key Derivative of Antitumor Drug Temozolomide. (2010) (0)
Spectroscopic Studies of the Interactions Between DNA and Novel Polycyclic Acridine Derivatives (1997) (0)
Structural Studies on Bioactive Compounds. Part 4. A Structure-Antitumor Activity Study on Analogues of N-Methylformamide. (1986) (0)
Thioredoxin-targeted experimental antitumor Quinols exert cytotoxicty following activation of apoptosis signal regulating kinase 1. (2007) (0)
TRIAZINES AND RELATED PRODUCTS. PART 26. SYNTHESIS AND CHEMISTRY OF BICYCLIC ANALOGS OF THE ANTITUMOR DRUG 2,4,6-TRIS(DIMETHYLAMINO)-1,3,5-TRIAZINE (HEXAMETHYLMELAMINE) (1984) (0)
The stability of n-hydroxymethyl compounds derived from n-methyl containing antitumour agents. Abstr. (1982) (0)
Antitumor Benzothiazoles. Part 9. The Regiospecific Synthesis of 5‐ and 7‐Monosubstituted and 5,6‐Disubstituted 2‐Arylbenzothiazoles. (2000) (0)
TRIAZINES AND RELATED PRODUCTS. PART 19. 4-AMINO-2(2-(PIPERIDIN-1-YLAZO)PHENYL)QUINAZOLINE AND ITS ANALOGS (1977) (0)
Decomposition of 2‐(4‐Azidophenyl)benzothiazoles (I) in Trifluoromethanesulfonic Acid (II): Formation of 2,2′‐Diaminobiphenyls (IV), (V). (1992) (0)
Medicinal nitro-compounds. 1. Photo-rearrangement of N-aryl-2-nitrobenzamides. (1973) (0)
Antitumor Polycyclic Acridines. Part 10. Synthesis of Penta‐ and Hexa‐cyclic Heteroaromatic Systems by Radical Cyclizations of Substituted 9‐Anilinoacridines. (2002) (0)
Triazines and related products. Part II. Heterolytic and homolytic decomposition of 1,3-di-o-cyanophenyltriazene (1968) (0)
Antitumour Activity and Pharmacology of CCRG 81010 (NSC 353451, M&B 39565, 8-carbamoyl-3-(1-chloroethyl)imidazo [5,1-d]-1,1,3,5-tetrazin-4(3H)-one) (1984) (0)
Antifolate pyrimidine compounds (1987) (0)
Structural Studies on Bioactive Compounds. Part 5. Synthesis and Properties of 2,4‐Diaminopyrimidine Dihydrofolate Reductase Inhibitors Bearing Lipophilic Azido Groups. (1988) (0)
CHEMISTRY OF HETEROCYCLIC COMPOUNDS. IX. TRIAZINES AND RELATED PRODUCTS. XVII. CYCLIZATION REACTIONS OF AZOLYLHYDRAZONES DERIVED FROM ETHYL CYANOACETATE AND MALONONITRILE. FORMATION OF AZOLO(5,1-C)(1,2,4)TRIAZINES (1976) (0)
TRIAZINES AND RELATED PRODUCTS. PART 20. OXIDATION OF 1-(ARYLAZO)PIPERIDINES WITH POTASSIUM PERMANGANATE (1977) (0)
Antitumor Polycyclic Acridines. Part 1. Synthesis of 7H-Pyrido- [cf. (IV)] and 8H-Quino-[4,3,2-kl]acridines [cf. (VII)] by Graebe—Ullmann Thermolysis of 9-(1,2,3-Triazol-1-yl)acridines: Application of Differential Scanning Calorimetry to Predict Optimum Cyclization Conditions. (1998) (0)
Condensed Benzimidazoles Bridged Between N‐1 and C‐7 (2008) (0)
Foerfarande Foer framstaellning of nya terapeutiskt anvaendbara / 3h / -imidazo / 5,1-d / -1,2,3,5, -tetrazin-derivative of 4-on. (1983) (0)
CCDC 1582899: Experimental Crystal Structure Determination (2018) (0)
TRIAZINES AND RELATED PRODUCTS. PART 23. NEW PHOTOPRODUCTS FROM 5-DIAZOIMIDAZOLE-4-CARBOXAMIDE (DIAZO-IC) (1981) (0)
Antitumor imidazotetrazinones: prodrugs targeted to the major groove of DNA. (1991) (0)
A New Route to the Antitumor Drug Temozolomide, But Not Thiotemozolomide. (1997) (0)
Reassignment of the Stereochemistry of Oblonginine. (1998) (0)
Structural Studies on Bioactive Compounds. Part 6. Determination of the Sites of Protonation on Three 2,4-Diaminopyrimidines of Pharmaceutical Importance by Proton-Coupled 13C and 1H NMR Spectroscopy. (1988) (0)
54 In vitro, in vivo and in silico examination of the activity of antitumor 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazoles (2004) (0)
Antitumor Benzothiazoles. Part 4. An NMR Study of the Sites of Protonation of 2‐(4‐Aminophenyl)benzothiazoles. (1996) (0)
TRIAZINES AND RELATED PRODUCTS. PART 30. CATIONIC ANALOGS OF THE ANTITUMOR DRUG 2,4,6-TRIS(DIMETHYLAMINO)-1,3,5-TRIAZINE (HEXAMETHYLMELAMINE) (1985) (0)
TRIAZINES AND RELATED PRODUCTS PART 11, DIMROTH REARRANGEMENTS OF 3-SUBSTITUTED 3,4-DIHYDRO-4-IMINO-1,2,3-BENZOTRIAZINES IN ACETIC ACID (1974) (0)
306 POSTER Aryl hydrocarbon receptor ligands 2-(3,4-dimethoxyphenyl)-fluorobenzothiazoles elicit potent and selective in vitro antitumor activity, inducing DNA damage that is independent of CYP1A1 bioactivation (2006) (0)
TRIAZINES AND RELATED PRODUCTS. PART XVI. SYNTHESIS OF TRIAZOLOTRIAZINES BY CYCLIZATION OF 3-HYDRAZINO-1,2,4-TRIAZINES AND 3-HYDRAZINO-1,2,4-TRIAZOLES (1976) (0)
A Revised Synthesis of the Antitumor Antibiotic L-Azatyrosine via 2-Iodo-5-methoxypyridine. (2002) (0)
Triazines and related products. 8. Potential irreversible chymotrypsin inhibitors: 3-alkyl-1,2,3-benzotriazin-4(3H)-ones and o-azidobenzamides. (1971) (0)
News imidazotetrazinones, their preparation and medicines containing them (1982) (0)
SELECTIVE REACTIONS IN THE TRIAZENE SERIES; I. REDUCTION OF 1-(4-ACETYLPHENYL)TRIAZENES (1983) (0)
Structural studies on bio-active compounds. Part 21. Acid-promoted debenzylations in antitumour 2,4-diamino-5-[4-(N-alkylbenzylamino)-3-nitrophenyl]-6-ethylp yrimidines. (1992) (0)
Antitumor Benzothiazoles. Part 2. Formation of 2,2′-Diaminobiphenyls from the Decomposition of 2-(4-Azidophenyl)benzazoles in Trifluoromethanesulfonic Acid. (2010) (0)
Structural Studies on Bio-active Compounds. Part 3. Re-examination of the Hydrolysis of the Antimalarial Drug Pyrimethamine and Related Derivatives and Crystal Structure of a Hydrolysis Product. (1986) (0)
MedChemComm Broadening the field of opportunity for medicinal chemists (2015) (0)
Photolysis of a methaqualone metabolite. (1972) (0)
Thiol-interactive antitumor quinols as modulators of cellular redox homeostasis (2005) (0)
Confirmation of the site of nitrosation in tryptophan derivatives by alpha-chymotrypsin. (1975) (0)
Foerfarande Foer of framstaellning / 3h / -imidazo- / 5,1-d / -1,2,3,5-Tetrazzini-4-onderivat with Terapeutisk Effect. (1982) (0)
Analogifremgangsmaade for preparing oe3haa-imidazo-oe5,1-DAA-1,2,3,5-tetrazine-4-one derivatives (1982) (0)
Pharmacokinetics in Mice of 8-Carbamoyl-3-methyl-imidazo [ 5 , l-onl , 2 , 3 , 5-tetrazin-4 ( 37 / )-one ( CCRG 81045 ; M & B 39831 ) , a Novel Drug with Potential as an Alternative to Dacarbazine 1 (2006) (0)
ENZYME INHIBITION STUDIES WITH DICHLOROBENZOPRIM: A NOVEL LIPOPHILIC ANTIFOLATE (1990) (0)
MEDICINAL NITRO-COMPOUNDS PART 2, SEARCH FOR ORTHO-INTERACTIONS IN TUMOUR-INHIBITORY 2,4-DINITROPHENYLAZIRIDINES (1975) (0)
α-HYDROXYLATED DERIVATIVES OF ANTITUMOR DIMETHYLTRIAZENES (1979) (0)
Introduction of a Triflate Group into Sterically Hindered Positions in 1‐Aryl‐4,6‐diamino‐1,3,5‐triazines and Their Dimroth Rearrangement Products. (1994) (0)
132 POSTER SRJ09, a lead compound in anticancer drug design: in vitro, in vivo and mechanistic studies (2008) (0)

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