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. Mortimer CG, Wells G, Crochard JP, Stone EL, Bradshaw TD, Stevens MF, Westwell AD. Journal of Medicinal Chemistry, 2006, 49, 179-185
The antitumor drug candidate 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole induced NF-kappa B activity in drug sensitive MCF-7 cells. Brantley E, Patel V, Stinson SF, Trapani V, Hose CD, Ciolino HP, Yeh GC, Gutkind JS, Sausvilee EA and Loaiza-Perez AI. Anti-cancer drugs, 2005, 16, 137-143.
Update to: The aryl hydrocarbon receptor in anticancer drug discovery: friend or foe. Bradshaw TD, Mortimer CG and Westwell AD. Medicinal Chemistry Reviews, 2005, in press.
The development of the antitumour benzothiazole prodrug, Phortress, as a clinical candidate. Bradshaw TD and Westwell AD. Current Medicinal Chemistry, 2004, 11, 1009-1023.
The experimental antitumor agents Phortress and Doxorubicin are equiactive against human-derived breast carcinoma xenograft models. Fichtner I, Monks A, Hose C, Stevens MFG and Bradshaw TD. Breast Cancer Research and Treatment, 2004, 87, 97-107.
In vitro, in vivo and in silico analyses of the antitumor activity of 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazoles. Leong C-O, Suggitt M, Swaine DJ, Bibby MC, Stevens MFG, Bradshaw TD. Molecular Cancer Therapeutic, 2004, 3 (12), 1565-1575.
The Therapeutic Potential of Aryl Hydrocarbon Receptor (AhR) Agonists in Anticancer Drug Development. Westwell AD. Drugs of the Future, 2004, 29(5), 479-491.
Fluorinated 2-(4-Amino-3-methylphenyl)benzothiazoles induce CYP1A1 expression, become metabolised, and bind to macromolecules in sensitive human cancer cells. Brantley E, Trapani V, Alley MC, Hose CD, Bradshaw TD, Stevens MFG, Sausville EA and Stinson SF. Drug Metabolism and Disposition, 2004, 32, 1392-1401.
The Development of the Antitumour Benzothiazole Prodrug, Phortress, as a Clinical Candidate. Bradshaw TD and Westwell AD. Curr. Med. Chem., 2004, 11, 1009-1021.
Antitumour Benzothiazoles. Part 20: 3´-Cyano and 3´-Alkynyl-Substituted 2-(4´-Aminophenyl)benzothiazoles as New Potent and Selective Analogues. Hutchinson I, Bradshaw TD, Matthews CS, Stevens MFG and Westwell AD. Bioorg. & Med. Chem. Lett., 2003, 13, 471-474.
Antitumour 2-(4-aminophenyl)benzothiazoles generate DNA adducts in sensitive tumour cells in vitro and in vivo. Leong C-O, Gaskell M, Martin EA, Heydon RT, Farmer PB, Bibby MC, Cooper PA, Double JA, Bradshaw TD, Stevens MFG. Brit. J. Cancer, 2003, 88, 470-477.