FIND

researchers

DISCOVER

relevant articles

PROMOTE

your research

now for free

Malcolm Stevens

Research Profile

Chemicals & Drugs

Concepts & Ideas

Anatomy

Co-author Network

Publications

TOP 3
Amy Capes; Iain T Collie; Alan H Fairlamb; Julie A Frearson; Irene Hallyburton; Andrew J McCarroll; Stephen Patterson; Malcolm F G Stevens; Paul G Wyatt; Susan Wyllie; Ian H Gilbert
Quinol derivatives as potential trypanocidal agents.
Jihong Zhang; Malcolm F G Stevens; Tracey D Bradshaw
Temozolomide: mechanisms of action, repair and resistance.
Boon Shing Tan; Kai Hung Tiong; Tracey D Bradshaw; Heng Lungh Choo; Ashwin Muruhadas; Nirmal Randhawa; Malcolm F G Stevens; Chee-Onn Leong
CYP2S1 and CYP2W1 mediate 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (GW-610, NSC 721648) sensitivity in breast and colorectal cancer cells.

Register for free to view:

Visualized networks:

See your personal network in
sophisticated graphical views

GeoTargeted Searches:

Locate experts around the world
and connect with global collaborators

Research Profiles:

See the research activity
of experts around the globe

Geonetwork of Malcolm Stevens (preview)

Cities where this author has publications
Cities where co-authors of this author have publications

Flash Player Required

All Publications

2012: Amy Capes; Iain T Collie; Alan H Fairlamb; Julie A Frearson; Irene Hallyburton; Andrew J McCarroll; Stephen Patterson; Malcolm F G Stevens; Paul G Wyatt; Susan Wyllie; Ian H Gilbert
Quinol derivatives as potential trypanocidal agents.
Bioorganic & medicinal chemistry 2012;20(4):1607-15.
2012: Jihong Zhang; Malcolm F G Stevens; Tracey D Bradshaw
Temozolomide: mechanisms of action, repair and resistance.
Current molecular pharmacology 2012;5(1):102-14.
2011: Boon Shing Tan; Kai Hung Tiong; Tracey D Bradshaw; Heng Lungh Choo; Ashwin Muruhadas; Nirmal Randhawa; Malcolm F G Stevens; Chee-Onn Leong
CYP2S1 and CYP2W1 mediate 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (GW-610, NSC 721648) sensitivity in breast and colorectal cancer cells.
Molecular cancer therapeutics 2011;10(10):1982-92.
2011: Annamaria Biroccio; Manuela Porru; Angela Rizzo; Erica Salvati; Carmen D'Angelo; Augusto Orlandi; Daniela Passeri; Marco Franceschin; Malcolm F G Stevens; Eric Gilson; Giovanni Beretta; Gabriella Zupi; Claudio Pisano; Franco Zunino; Carlo Leonetti
DNA damage persistence as determinant of tumor sensitivity to the combination of Topo I inhibitors and telomere-targeting agents.
Clinical cancer research : an official journal of the American Association for Cancer Research 2011;17(8):2227-36.
2011: Jihong Zhang; Marc Geoffery Hummersone; Charles A Laughton; Srinivasan Madhusudan; Malcolm F G Stevens; Tracey D Bradshaw
Certain imidazotetrazines escape O6-methylguanine-DNA methyltransferase and mismatch repair.
Oncology 2011;80(3-4):195-207.
2010: E Salvati; Marco Scarsella; M Porru; A Rizzo; S Iachettini; L Tentori; G Graziani; Maurizio D'Incalci; Malcolm F G Stevens; A Orlandi; D Passeri; Eric Gilson; Gabriella Zupi; Carlo Leonetti; Annamaria Biroccio
PARP1 is activated at telomeres upon G4 stabilization: possible target for telomere-based therapy.
Oncogene 2010;29(47):6280-93.
2010: Andrew J McCarroll; Charles S Matthews; Geoffrey Wells; Tracey D Bradshaw; Malcolm F G Stevens
Synthesis of antitumour (1H-1,2,3-triazol-4-yl)-4-hydroxycyclohexa-2,5-dien-1-ones by copper-catalysed Huisgen cycloadditions.
Organic & biomolecular chemistry 2010;8(9):2078-84.
2010: Jihong Zhang; Malcolm F G Stevens; Charles A Laughton; Srinivasan Madhusudan; Tracey D Bradshaw
Acquired resistance to temozolomide in glioma cell lines: molecular mechanisms and potential translational applications.
Oncology 2010;78(2):103-14.
2009: Matthew R Smith; Alexander J Blake; Christopher J Hayes; Malcolm F G Stevens; Christopher J Moody
Carbene reactivity of 4-diazo-4H-imidazoles toward nucleophiles and aromatic compounds.
The Journal of organic chemistry 2009;74(24):9372-80.
2009: Thomas P Garner; Huw E L Williams; Katarzyna I Gluszyk; Stephen Roe; Neil J Oldham; Malcolm F G Stevens; John E Moses; Mark S Searle
Selectivity of small molecule ligands for parallel and anti-parallel DNA G-quadruplex structures.
Organic & biomolecular chemistry 2009;7(20):4194-200.
2009: Rana Bazzi; Tracey D Bradshaw; Craig Rowlands; Malcolm F G Stevens; David R Bell
2-(4-Amino-3-methylphenyl)-5-fluorobenzothiazole is a ligand and shows species-specific partial agonism of the aryl hydrocarbon receptor.
Toxicology and applied pharmacology 2009;237(1):102-10.
2009: Tracey D Bradshaw; J E Wren; M Bruce; David A Barrett; Chee-Onn Leong; Margaret Gaskell; E K Wright; Peter B Farmer; Colin Henderson; R Wolf; Malcolm F G Stevens
Preclinical toxicokinetic evaluation of phortress [2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole lysylamide dihydrochloride] in two rodent species.
Pharmacology 2009;83(2):99-109.
2008: Carlo Leonetti; Marco Scarsella; Giuseppe Riggio; Angela Rizzo; Erica Salvati; Maurizio D'Incalci; Lidia Staszewsky; Roberta Frapolli; Malcolm F G Stevens; Antonella Stoppacciaro; Marcella Mottolese; Barbara Antoniani; Eric Gilson; Gabriella Zupi; Annamaria Biroccio
G-quadruplex ligand RHPS4 potentiates the antitumor activity of camptothecins in preclinical models of solid tumors.
Clinical cancer research : an official journal of the American Association for Cancer Research 2008;14(22):7284-91.
2008: Srinivasa Rao Jada; C Matthews; Mohammad Said Saad; Ahmad Sazali Hamzah; Nordin Hj Lajis; Malcolm F G Stevens; Johnson Stanslas
Benzylidene derivatives of andrographolide inhibit growth of breast and colon cancer cells in vitro by inducing G(1) arrest and apoptosis.
British journal of pharmacology 2008;155(5):641-54.
2008: Hachemi Kadri; Charles S Matthews; Tracey D Bradshaw; Malcolm F G Stevens; Andrew D Westwell
Synthesis and antitumour evaluation of novel 2-phenylbenzimidazoles.
Journal of enzyme inhibition and medicinal chemistry 2008;23(5):641-7.
2008: Stefania Aiello; Geoffrey Wells; Erica Stone; Hachemi Kadri; Rana Bazzi; David R Bell; Malcolm F G Stevens; Charles S Matthews; Tracey D Bradshaw; Andrew D Westwell
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).
Journal of medicinal chemistry 2008;51(16):5135-9.
2008: Tracey D Bradshaw; Erica Stone; Valentina Trapani; Chee-Onn Leong; Charles S Matthews; Robert te Poele; Malcolm F G Stevens
Mechanisms of acquired resistance to 2-(4-Amino-3-methylphenyl)benzothiazole in breast cancer cell lines.
Breast cancer research and treatment 2008;110(1):57-68.
2008: Mai-Kim Cheng; Chetna Modi; Jennifer C Cookson; Ian Hutchinson; Robert A Heald; Andrew J McCarroll; Sotiris Missailidis; Farial Tanious; David W. Wilson; Jean-Louis Mergny; Charles A Laughton; Malcolm F G Stevens
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.
Journal of medicinal chemistry 2008;51(4):963-75.
2007: Erica Salvati; Carlo Leonetti; Angela Rizzo; Marco Scarsella; Marcella Mottolese; rossella galati; Isabella Sperduti; Malcolm F G Stevens; Maurizio D'Incalci; Maria Blasco; giovanna chiorino; Serge Bauwens; Béatrice Horard; Eric Gilson; Antonella Stoppacciaro; Gabriella Zupi; Annamaria Biroccio
Telomere damage induced by the G-quadruplex ligand RHPS4 has an antitumor effect.
The Journal of clinical investigation 2007;117(11):3236-47.
2007: Pornima Phatak; Jennifer C Cookson; F Dai; V Smith; Ronald B Gartenhaus; Malcolm F G Stevens; Angelika Burger
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.
British journal of cancer 2007;96(8):1223-33.
2007: Andrew J McCarroll; Tracey D Bradshaw; Andrew D Westwell; Charles S Matthews; Malcolm F G Stevens
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.
Journal of medicinal chemistry 2007;50(7):1707-10.
2007: Srinivasa Rao Jada; Genevieve Suseno Subur; Charlie Matthews; Ahmad Sazali Hamzah; Nordin Hj Lajis; Mohammad Said Saad; Malcolm F G Stevens; Johnson Stanslas
Semisynthesis and in vitro anticancer activities of andrographolide analogues.
Phytochemistry 2007;68(6):904-12.
2007: Ian Hutchinson; Malcolm F G Stevens
Synthetic strategies to a telomere-targeted pentacyclic heteroaromatic salt.
Organic & biomolecular chemistry 2007;5(1):114-20.
2006: Cedric J Lion; Charles S Matthews; Geoffrey Wells; Tracey D Bradshaw; Malcolm F G Stevens; Andrew D Westwell
Antitumour properties of fluorinated benzothiazole-substituted hydroxycyclohexa-2,5-dienones ('quinols').
Bioorganic & medicinal chemistry letters 2006;16(19):5005-8.
2006: Dylan T Jones; Christopher W Pugh; Simon Wigfield; Malcolm F G Stevens; Adrian L Harris
Novel thioredoxin inhibitors paradoxically increase hypoxia-inducible factor-alpha expression but decrease functional transcriptional activity, DNA binding, and degradation.
Clinical cancer research : an official journal of the American Association for Cancer Research 2006;12(18):5384-94.
2006: Annamaria Biroccio; Angela Rizzo; Raffaella Elli; Catherine-Elaine Koering; Aurélie Belleville; Barbara Benassi; Carlo Leonetti; Malcolm F G Stevens; Maurizio D'Incalci; Gabriella Zupi; Eric Gilson
TRF2 inhibition triggers apoptosis and reduces tumourigenicity of human melanoma cells.
European journal of cancer (Oxford, England : 1990) 2006;42(12):1881-8.
2006: Eng-Hui Chew; Charles S Matthews; Jihong Zhang; Andrew J McCarroll; Thilo Hagen; Malcolm F G Stevens; Andrew D Westwell; Tracey D Bradshaw
Antitumor quinols: role of glutathione in modulating quinol-induced apoptosis and identification of putative cellular protein targets.
Biochemical and biophysical research communications 2006;346(1):242-51.
2006: David A Vasselin; Andrew D Westwell; Charles S Matthews; Tracey D Bradshaw; Malcolm F G Stevens
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.
Journal of medicinal chemistry 2006;49(13):3973-81.
2006: Srinivasa Rao Jada; Ahmad Sazali Hamzah; Nordin Hj Lajis; Mohammad Said Saad; Malcolm F G Stevens; Johnson Stanslas
Semisynthesis and cytotoxic activities of andrographolide analogues.
Journal of enzyme inhibition and medicinal chemistry 2006;21(2):145-55.
2006: Catriona G Mortimer; Geoffrey Wells; Jean-Philippe Crochard; Erica Stone; Tracey D Bradshaw; Malcolm F G Stevens; Andrew D Westwell
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.
Journal of medicinal chemistry 2006;49(1):179-85.
2005: Jennifer C Cookson; Fangping Dai; Victoria Smith; Robert A Heald; Charles A Laughton; Malcolm F G Stevens; Angelika Burger
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.
Molecular pharmacology 2005;68(6):1551-8.
2005: Jennifer C Cookson; Robert A Heald; Malcolm F G Stevens
Antitumor polycyclic acridines. 17. Synthesis and pharmaceutical profiles of pentacyclic acridinium salts designed to destabilize telomeric integrity.
Journal of medicinal chemistry 2005;48(23):7198-207.
2005: Cedric J Lion; David A Vasselin; Carl H Schwalbe; Charles S Matthews; Malcolm F G Stevens; Andrew D Westwell
Novel reaction products from the hypervalent iodine oxidation of hydroxylated stilbenes and isoflavones.
Organic & biomolecular chemistry 2005;3(21):3996-4001.
2005: Tracey D Bradshaw; Charles S Matthews; Jennifer C Cookson; Eng-Hui Chew; Manish Shah; Kevin Bailey; Anne Monks; Erik Harris; Andrew D Westwell; Geoffrey Wells; Charles A Laughton; Malcolm F G Stevens
Elucidation of thioredoxin as a molecular target for antitumor quinols.
Cancer research 2005;65(9):3911-9.
2005: Cedric J Lion; Charles S Matthews; Malcolm F G Stevens; Andrew D Westwell
Synthesis, antitumor evaluation, and apoptosis-inducing activity of hydroxylated (E)-stilbenes.
Journal of medicinal chemistry 2005;48(4):1292-5.
2005: A Mukherjee; Andrew D Westwell; Tracey D Bradshaw; Malcolm F G Stevens; James Carmichael; Stewart Graham Martin
Cytotoxic and antiangiogenic activity of AW464 (NSC 706704), a novel thioredoxin inhibitor: an in vitro study.
British journal of cancer 2005;92(2):350-8.
2005: Jane M Berry; Tracey D Bradshaw; Iduna Fichtner; Ruobo Ren; Carl H Schwalbe; Geoffrey Wells; Eng-Hui Chew; Malcolm F G Stevens; Andrew D Westwell
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.
Journal of medicinal chemistry 2005;48(2):639-44.
2005: Sotiris Missailidis; Chetna Modi; Valentina Trapani; Charles A Laughton; Malcolm F G Stevens
Antitumor polycyclic acridines. Part 16. Triplex DNA as a target for DNA-binding polycyclic acridine derivatives.
Oncology research 2005;15(2):95-105.
2004: Chee-Onn Leong; Marie Suggitt; David J Swaine; Michael C Bibby; Malcolm F G Stevens; Tracey D Bradshaw
In vitro, in vivo, and in silico analyses of the antitumor activity of 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazoles.
Molecular cancer therapeutics 2004;3(12):1565-75.
2004: Eileen Brantley; Valentina Trapani; Michael C Alley; Curtis Hose; Tracey D Bradshaw; Malcolm F G Stevens; Edward A Sausville; Sherman F Stinson
Fluorinated 2-(4-amino-3-methylphenyl)benzothiazoles induce CYP1A1 expression, become metabolized, and bind to macromolecules in sensitive human cancer cells.
Drug metabolism and disposition: the biological fate of chemicals 2004;32(12):1392-401.
2004: Carlo Leonetti; Sarah Amodei; Carmen D'Angelo; Angela Rizzo; Barbara Benassi; Anna Antonelli; Raffaella Elli; Malcolm F G Stevens; Maurizio D'Incalci; Gabriella Zupi; Annamaria Biroccio
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.
Molecular pharmacology 2004;66(5):1138-46.
2004: Iduna Fichtner; Anne Monks; Curtis Hose; Malcolm F G Stevens; Tracey D Bradshaw
The experimental antitumor agents Phortress and doxorubicin are equiactive against human-derived breast carcinoma xenograft models.
Breast cancer research and treatment 2004;87(1):97-107.
2004: Andrew D Westwell; Malcolm F G Stevens
Hitting the chemotherapy jackpot: strategy, productivity and chemistry.
Drug discovery today 2004;9(15):625-7.
2004: Marianne L Richardson; Karen A Croughton; Charles S Matthews; Malcolm F G Stevens
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').
Journal of medicinal chemistry 2004;47(16):4105-8.
2004: Mark S Searle; Huw E L Williams; Cathal T Gallagher; Richard J Grant; Malcolm F G Stevens
Structure and K+ ion-dependent stability of a parallel-stranded DNA quadruplex containing a core A-tetrad.
Organic & biomolecular chemistry 2004;2(6):810-2.
2004: Ian Hutchinson; Andrew J McCarroll; Robert A Heald; Malcolm F G Stevens
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.
Organic & biomolecular chemistry 2004;2(2):220-8.
2003: Evripidis Gavathiotis; Robert A Heald; Malcolm F G Stevens; Mark S Searle
Drug recognition and stabilisation of the parallel-stranded DNA quadruplex d(TTAGGGT)4 containing the human telomeric repeat.
Journal of molecular biology 2003;334(1):25-36.
2003: Monica Pallis; Tracey D Bradshaw; Andrew D Westwell; Martin Grundy; Malcolm F G Stevens; Nigel Russell
Induction of apoptosis without redox catastrophe by thioredoxin-inhibitory compounds.
Biochemical pharmacology 2003;66(9):1695-705.
2003: Robert A Heald; Malcolm F G Stevens
Antitumour polycyclic acridines. Palladium(0) mediated syntheses of quino[4,3,2-kl]acridines bearing peripheral substituents as potential telomere maintenance inhibitors.
Organic & biomolecular chemistry 2003;1(19):3377-89.
2003: Azeem Saleem; Gavin D Brown; Frank Brady; Eric O Aboagye; Safiye Osman; Sajinder K Luthra; Alex S Ranicar; Cathryn S Brock; Malcolm F G Stevens; Edward S Newlands; Terry Jones; Pat Price
Metabolic activation of temozolomide measured in vivo using positron emission tomography.
Cancer research 2003;63(10):2409-15.
2003: Valentina Trapani; Vyomesh Patel; Chee-Onn Leong; Henry P Ciolino; Grace Chao Yeh; Curtis Hose; Jane Trepel; Malcolm F G Stevens; Edward A Sausville; Andrea I Loaiza-Pérez
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.
British journal of cancer 2003;88(4):599-605.
2003: Geoffrey Wells; Jane M Berry; Tracey D Bradshaw; Angelika Burger; Angela Seaton; Bo Wang; Andrew D Westwell; Malcolm F G Stevens
4-Substituted 4-hydroxycyclohexa-2,5-dien-1-ones with selective activities against colon and renal cancer cell lines.
Journal of medicinal chemistry 2003;46(4):532-41.
2003: Chee-Onn Leong; Margaret Gaskell; E A Martin; RT Heydon; Peter B Farmer; Michael C Bibby; Patricia A Cooper; John A Double; Tracey D Bradshaw; Malcolm F G Stevens
Antitumour 2-(4-aminophenyl)benzothiazoles generate DNA adducts in sensitive tumour cells in vitro and in vivo.
British journal of cancer 2003;88(3):470-7.
2003: Ian Hutchinson; Tracey D Bradshaw; Charles S Matthews; Malcolm F G Stevens; Andrew D Westwell
Antitumour benzothiazoles. Part 20: 3'-cyano and 3'-alkynyl-substituted 2-(4'-aminophenyl)benzothiazoles as new potent and selective analogues.
Bioorganic & medicinal chemistry letters 2003;13(3):471-4.
2003: Sean E O'Brien; Helen L Browne; Tracey D Bradshaw; Andrew D Westwell; Malcolm F G Stevens; Charles A Laughton
Antitumor benzothiazoles. Frontier molecular orbital analysis predicts bioactivation of 2-(4-aminophenyl)benzothiazoles to reactive intermediates by cytochrome P4501A1.
Organic & biomolecular chemistry 2003;1(3):493-7.
2002: Jill Arrowsmith; Sharon A Jennings; Alan S Clark; Malcolm F G Stevens
Antitumor imidazotetrazines. 41. Conjugation of the antitumor agents mitozolomide and temozolomide to peptides and lexitropsins bearing DNA major and minor groove-binding structural motifs.
Journal of medicinal chemistry 2002;45(25):5458-70.
2002: Gavin D Brown; Sajinder K Luthra; Cathryn S Brock; Malcolm F G Stevens; Patricia M Price; Frank Brady
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.
Journal of medicinal chemistry 2002;45(25):5448-57.
2002: David C M Chan; Charles A Laughton; Sherry F Queener; Malcolm F G Stevens
Structural studies on bioactive compounds. Part 36: design, synthesis and biological evaluation of pyrimethamine-based antifolates against Pneumocystis carinii.
Bioorganic & medicinal chemistry 2002;10(9):3001-10.
2002: Tracey D Bradshaw; MS Chua; Helen L Browne; Valentina Trapani; Edward A Sausville; Malcolm F G Stevens
In vitro evaluation of amino acid prodrugs of novel antitumour 2-(4-amino-3-methylphenyl)benzothiazoles.
British journal of cancer 2002;86(8):1348-54.
2002: Tracey D Bradshaw; Michael C Bibby; John A Double; Iduna Fichtner; Patricia A Cooper; Michael C Alley; Susan Donohue; Sherman F Stinson; Joseph E Tomaszewjski; Edward A Sausville; Malcolm F G Stevens
Preclinical evaluation of amino acid prodrugs of novel antitumor 2-(4-amino-3-methylphenyl)benzothiazoles.
Molecular cancer therapeutics 2002;1(4):239-46.
2002: Ian Hutchinson; Sharon A Jennings; B Rao Vishnuvajjala; Andrew D Westwell; Malcolm F G Stevens
Antitumor benzothiazoles. 16. Synthesis and pharmaceutical properties of antitumor 2-(4-aminophenyl)benzothiazole amino acid prodrugs.
Journal of medicinal chemistry 2002;45(3):744-7.
2002: Robert A Heald; Chetna Modi; Jennifer C Cookson; Ian Hutchinson; Charles A Laughton; Sharon M Gowan; Lloyd R Kelland; Malcolm F G Stevens
Antitumor polycyclic acridines. 8.(1) Synthesis and telomerase-inhibitory activity of methylated pentacyclic acridinium salts.
Journal of medicinal chemistry 2002;45(3):590-7.
2002: Sotiris Missailidis; Johnson Stanslas; Chetna Modi; Michael J Ellis; R Adrian Robins; Charles A Laughton; Malcolm F G Stevens
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.
Oncology research 2002;13(3):175-89.
2002: Andrea I Loaiza-Pérez; Valentina Trapani; Curtis Hose; Sheo S Singh; Jane Trepel; Malcolm F G Stevens; Tracey D Bradshaw; Edward A Sausville
Aryl hydrocarbon receptor mediates sensitivity of MCF-7 breast cancer cells to antitumor agent 2-(4-amino-3-methylphenyl) benzothiazole.
Molecular pharmacology 2002;61(1):13-9.
2001: D C Chan; Charles A Laughton; Sherry F Queener; Malcolm F G Stevens
Structural studies on bioactive compounds. 34. Design, synthesis, and biological evaluation of triazenyl-substituted pyrimethamine inhibitors of Pneumocystis carinii dihydrofolate reductase.
Journal of medicinal chemistry 2001;44(16):2555-64.
2001: Ian Hutchinson; MS Chua; Helen L Browne; Valentina Trapani; Tracey D Bradshaw; Andrew D Westwell; Malcolm F G Stevens
Antitumor benzothiazoles. 14. Synthesis and in vitro biological properties of fluorinated 2-(4-aminophenyl)benzothiazoles.
Journal of medicinal chemistry 2001;44(9):1446-55.
2001: DF Shi; Tracey D Bradshaw; MS Chua; Andrew D Westwell; Malcolm F G Stevens
Antitumour benzothiazoles. Part 15: The synthesis and physico-chemical properties of 2-(4-aminophenyl)benzothiazole sulfamate salt derivatives.
Bioorganic & medicinal chemistry letters 2001;11(8):1093-5.
2001: K A Croughton; Charles S Matthews; R J Griffin; Malcolm F G Stevens
Investigations on the biological properties of the lipophilic DHFR-inhibitory benzoprims reveal non-folate modes of action and opportunities for anti-cancer drug design.
Anti-cancer drug design 2001;16(2-3):119-28.
2001: Tracey D Bradshaw; Malcolm F G Stevens; Andrew D Westwell
The discovery of the potent and selective antitumour agent 2-(4-amino-3-methylphenyl)benzothiazole (DF 203) and related compounds.
Current medicinal chemistry 2001;8(2):203-10.
2000: MS Chua; E Kashiyama; Tracey D Bradshaw; Sherman F Stinson; Eileen Brantley; Edward A Sausville; Malcolm F G Stevens
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.
Cancer research 2000;60(18):5196-203.
2000: Tracey D Bradshaw; MS Chua; S Orr; Charles S Matthews; Malcolm F G Stevens
Mechanisms of acquired resistance to 2-(4-aminophenyl)benzothiazole (CJM 126, NSC 34445).
British journal of cancer 2000;83(2):270-7.
2000: Johnson Stanslas; D J Hagan; M J Ellis; C Turner; James Carmichael; Wynne Ward; T R Hammonds; Malcolm F G Stevens
Antitumor polycyclic acridines. 7. Synthesis and biological properties of DNA affinic tetra- and pentacyclic acridines.
Journal of medicinal chemistry 2000;43(8):1563-72.
2000: Geoffrey Wells; Angela Seaton; Malcolm F G Stevens
Structural studies on bioactive compounds. 32. Oxidation of tyrphostin protein tyrosine kinase inhibitors with hypervalent iodine reagents.
Journal of medicinal chemistry 2000;43(8):1550-62.
2000: D R Hannah; E C Sherer; R V Davies; R B Titman; Charles A Laughton; Malcolm F G Stevens
Structural studies on bioactive compounds. Part 29: palladium catalysed arylations and alkynylations of sterically hindered immunomodulatory 2-amino-5-halo-4,6-(disubstituted)pyrimidines.
Bioorganic & medicinal chemistry 2000;8(4):739-50.
2000: Geoffrey Wells; Tracey D Bradshaw; P Diana; Angela Seaton; DF Shi; Andrew D Westwell; Malcolm F G Stevens
Antitumour benzothiazoles. Part 10: the synthesis and antitumour activity of benzothiazole substituted quinol derivatives.
Bioorganic & medicinal chemistry letters 2000;10(5):513-5.
1999: E Kashiyama; Ian Hutchinson; MS Chua; Sherman F Stinson; LR Phillips; G Kaur; Edward A Sausville; Tracey D Bradshaw; Andrew D Westwell; Malcolm F G Stevens
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
Journal of medicinal chemistry 1999;42(20):4172-84.
1999: J Arrowsmith; Sotiris Missailidis; Malcolm F G Stevens
Antitumour imidazotetrazines. Part 37. Conjugation of the DNA major-groove alkylating imidazotetrazine mitozolomide to peptide motifs recognizing the minor groove.
Anti-cancer drug design 1999;14(3):205-17.
1999: CE Bostock-Smith; E Giménez-Arnau; Sotiris Missailidis; Charles A Laughton; Malcolm F G Stevens; Mark S Searle
Molecular recognition between a new pentacyclic acridinium salt and DNA sequences investigated by optical spectroscopic techniques, proton nuclear magnetic resonance spectroscopy, and molecular modeling.
Biochemistry 1999;38(21):6723-31.
1999: MS Chua; DF Shi; S Wrigley; Tracey D Bradshaw; Ian Hutchinson; P Nicholas Shaw; David A Barrett; L A Stanley; Malcolm F G Stevens
Antitumor benzothiazoles. 7. Synthesis of 2-(4-acylaminophenyl)benzothiazoles and investigations into the role of acetylation in the antitumor activities of the parent amines.
Journal of medicinal chemistry 1999;42(3):381-92.
1998: Tracey D Bradshaw; DF Shi; R J Schultz; K D Paull; Lloyd R Kelland; A Wilson; C Garner; H H Fiebig; S Wrigley; Malcolm F G Stevens
Influence of 2-(4-aminophenyl)benzothiazoles on growth of human ovarian carcinoma cells in vitro and in vivo.
British journal of cancer 1998;78(4):421-9.
1998: E Giménez-Arnau; Sotiris Missailidis; Malcolm F G Stevens
Antitumour polycyclic acridines. Part 4. Physico-chemical studies on the interactions between DNA and novel tetracyclic acridine derivatives.
Anti-cancer drug design 1998;13(5):431-51.
1998: E Giménez-Arnau; Sotiris Missailidis; Malcolm F G Stevens
Antitumour polycyclic acridines. Part 2. Physicochemical studies on the interactions between DNA and novel polycyclic acridine derivatives.
Anti-cancer drug design 1998;13(2):125-43.
1998: Tracey D Bradshaw; S Wrigley; DF Shi; R J Schultz; K D Paull; Malcolm F G Stevens
2-(4-Aminophenyl)benzothiazoles: novel agents with selective profiles of in vitro anti-tumour activity.
British journal of cancer 1998;77(5):745-52.
1997: Malcolm F G Stevens; K S Phillip; Daniel L Rathbone; D M O'Shea; Sherry F Queener; Carl H Schwalbe; PA Lambert
Structural studies on bioactive compounds. 28. Selective activity of triazenyl-substituted pyrimethamine derivatives against Pneumocystis carinii dihydrofolate reductase.
Journal of medicinal chemistry 1997;40(12):1886-93.
1996: DF Shi; Tracey D Bradshaw; S Wrigley; C J McCall; P Lelieveld; I Fichtner; Malcolm F G Stevens
Antitumor benzothiazoles. 3. Synthesis of 2-(4-aminophenyl)benzothiazoles and evaluation of their activities against breast cancer cell lines in vitro and in vivo.
Journal of medicinal chemistry 1996;39(17):3375-84.
1995: A S Clark; B Deans; Malcolm F G Stevens; Michael J Tisdale; R T Wheelhouse; B J Denny; John A Hartley
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
Journal of medicinal chemistry 1995;38(9):1493-504.
1995: Malcolm F G Stevens; G U Baig; E N Gate; R T Wheelhouse
Structural studies on bioactive compounds. Part 27. Chemistry of the immunomodulatory agent bropirimine.
Anti-cancer drug design 1995;10(3):215-26.
1995: Malcolm F G Stevens; C H Schwalbe; N Patel; E N Gate; P K Bryant
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.
Anti-cancer drug design 1995;10(3):203-13.
1994: B J Denny; R T Wheelhouse; Malcolm F G Stevens; L L Tsang; J A Slack
NMR and molecular modeling investigation of the mechanism of activation of the antitumor drug temozolomide and its interaction with DNA.
Biochemistry 1994;33(31):9045-51.
1994: Malcolm F G Stevens; C J McCall; P Lelieveld; P Alexander; A Richter; D E Davies
Structural studies on bioactive compounds. 23. Synthesis of polyhydroxylated 2-phenylbenzothiazoles and a comparison of their cytotoxicities and pharmacological properties with genistein and quercetin.
Journal of medicinal chemistry 1994;37(11):1689-95.
1993: Malcolm F G Stevens; E S Newlands
From triazines and triazenes to temozolomide.
European journal of cancer (Oxford, England : 1990) 1993;29A(7):1045-7.
1992: Roger J Griffin; Malcolm F G Stevens
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.
Anti-cancer drug design 1992;7(6):443-9.
1992: P R Lowe; C E Sansom; C H Schwalbe; Malcolm F G Stevens; A S Clark
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.
Journal of medicinal chemistry 1992;35(18):3377-82.
1992: B J Denny; N S Ringan; C H Schwalbe; Peter A Lambert; M A Meek; Roger J Griffin; Malcolm F G Stevens
Structural studies on bio-active compounds. 20. Molecular modeling and crystallographic studies on methylbenzoprim, a potent inhibitor of dihydrofolate reductase.
Journal of medicinal chemistry 1992;35(12):2315-20.
1992: Edward S Newlands; George Blackledge; J A Slack; Gordon J S Rustin; D B Smith; N S Stuart; C P Quarterman; R Hoffman; Malcolm F G Stevens; MH Brampton
Phase I trial of temozolomide (CCRG 81045: M&B 39831: NSC 362856).
British journal of cancer 1992;65(2):287-91.
1991: Malcolm F G Stevens
Antitumor imidazotetrazinones: prodrugs targeted to the major groove of DNA.
Farmaco (Società chimica italiana : 1989) 1991;46(1 Suppl):147-59.
1990: C E Sansom; Charles A Laughton; S Neidle; C H Schwalbe; Malcolm F G Stevens
Structural studies on bio-active compounds. Part XIV. Molecular modelling of the interactions between pentamidine and DNA.
Anti-cancer drug design 1990;5(3):243-8.
1990: Keith R Fox; C E Sansom; Malcolm F G Stevens
Footprinting studies on the sequence-selective binding of pentamidine to DNA.
FEBS letters 1990;266(1-2):150-4.
1990: Roger J Griffin; Malcolm F G Stevens; C E Sansom
Structural studies on bio-active compounds. Part 16. Synthesis and properties of sterically-constrained analogues of methylbenzoprim, a new dihydrofolate reductase inhibitor.
Anti-cancer drug design 1990;5(2):201-11.
1990: K R Horspool; Malcolm F G Stevens; C G Newton; E Lunt; R J Walsh; B L Pedgrift; G U Baig; F Lavelle; C Fizames
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
Journal of medicinal chemistry 1990;33(5):1393-9.
1990: A S Clark; Malcolm F G Stevens; C E Sansom; C H Schwalbe
Anti-tumour imidazotetrazines. Part XXI. Mitozolomide and temozolomide: probes for the major groove of DNA.
Anti-cancer drug design 1990;5(1):63-8.
1990: David J Kerr; J A Slack; P Secrett; Malcolm F G Stevens; George Blackledge; C Bradley; Stanley B Kaye
Relationship between the pharmacokinetics and toxicity of mitozolomide.
Cancer chemotherapy and pharmacology 1990;25(5):352-4.
1989: Roger J Griffin; M A Meek; C H Schwalbe; Malcolm F G Stevens
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.
Journal of medicinal chemistry 1989;32(11):2468-74.
1989: K R Horspool; C P Quarterman; J A Slack; A Gescher; Malcolm F G Stevens; E Lunt
Metabolism and murine pharmacokinetics of the 8-(N,N-dimethylcarboxamide) analogue of the experimental antitumor drug mitozolomide (NSC353451).
Cancer research 1989;49(18):5023-6.
1989: C E Sansom; C H Schwalbe; Peter A Lambert; Roger J Griffin; Malcolm F G Stevens
Structural studies on bio-active compounds. Part XV. Structure-activity relationships for pyrimethamine and a series of diaminopyrimidine analogues versus bacterial dihydrofolate reductase.
Biochimica et biophysica acta 1989;995(1):21-7.
1989: N S Stuart; S M Crawford; George Blackledge; Edward S Newlands; J Slack; R Hoffman; Malcolm F G Stevens
A phase I study of meta-azidopyrimethamine ethanesulphonate (MZPES)--a new dihydrofolate reductase inhibitor.
Cancer chemotherapy and pharmacology 1989;23(5):308-10.
1987: Malcolm F G Stevens; Roger J Griffin; S K Wong
The aromatic azido group in anti-cancer drug design: application in the development of novel lipophilic dihydrofolate reductase inhibitors.
Anti-cancer drug design 1987;2(3):311-8.
1987: C H Schwalbe; M E King; K P Wong; Peter A Lambert; A Bliss; Malcolm F G Stevens
Structural studies on bio-active compounds. Part 9. 2,4-Diamino-6-azidoquinazoline hydrochloride.
Anti-cancer drug design 1987;2(3):289-96.
1987: Malcolm F G Stevens; J A Hickman; S P Langdon; D Chubb; L Vickers; R Stone; G Baig; C Goddard; N W Gibson; J A Slack
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.
Cancer research 1987;47(22):5846-52.
1987: E Lunt; C G Newton; C Smith; G P Stevens; Malcolm F G Stevens; C G Straw; R J Walsh; P J Warren; C Fizames; F Lavelle
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.
Journal of medicinal chemistry 1987;30(2):357-66.
1986: E N Gate; Michael Threadgill; Malcolm F G Stevens; D Chubb; L M Vickers; S P Langdon; J A Hickman; A Gescher
Structural studies on bioactive compounds. 4. A structure-antitumor activity study on analogues of N-methylformamide.
Journal of medicinal chemistry 1986;29(6):1046-52.
1985: E S Newlands; G Blackledge; J A Slack; C Goddard; C J Brindley; L Holden; Malcolm F G Stevens
Phase I clinical trial of mitozolomide.
Cancer treatment reports 1985;69(7-8):801-5.
1985: C Goddard; J A Slack; Malcolm F G Stevens
Antitumour imidazotetrazines, Part IX. The pharmacokinetics of mitozolomide in mice.
British journal of cancer 1985;52(1):37-41.
1985: J A Hickman; Malcolm F G Stevens; N W Gibson; S P Langdon; C Fizames; F Lavelle; G Atassi; E Lunt; R M Tilson
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.
Cancer research 1985;45(7):3008-13.
1985: S P Langdon; J A Hickman; A Gescher; Malcolm F G Stevens; D Chubb; L M Vickers
N-Methylformamide (NSC 3051): a potential candidate for combination chemotherapy.
European journal of cancer & clinical oncology 1985;21(6):745-52.
1985: S P Langdon; D Chubb; A Gescher; J A Hickman; Malcolm F G Stevens
Studies on the toxicity of the antitumour agent N-methylformamide in mice.
Toxicology 1985;34(2):173-83.
1984: S P Langdon; A Gescher; J A Hickman; Malcolm F G Stevens
The chemosensitivity of a new experimental model--the M5076 reticulum cell sarcoma.
European journal of cancer & clinical oncology 1984;20(5):699-705.
1984: D Ross; S P Langdon; A Gescher; Malcolm F G Stevens
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.
Biochemical pharmacology 1984;33(7):1131-6.
1984: Malcolm F G Stevens; J A Hickman; R Stone; N W Gibson; G U Baig; E Lunt; C G Newton
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.
Journal of medicinal chemistry 1984;27(2):196-201.
1983: P G Cooksey; E N Gate; A Gescher; J A Hickman; S P Langdon; Malcolm F G Stevens
The formation and metabolism of N-hydroxymethyl compounds--IV. Cytotoxicity and antitumour activity of N-hydroxymethylformamide, a putative metabolite of N-methylformamide (NSC 3051).
Biochemical pharmacology 1983;32(20):3037-43.