The Discovery of the Potent and Selective Antitumour Agent 2-(4-Amino-3-methylphenyl)benzothiazole (DF 203) and Related Compounds

Title: The Discovery of the Potent and Selective Antitumour Agent 2-(4-Amino-3-methylphenyl)benzothiazole (DF 203) and Related Compounds

Volume: 8 Issue: 2

Author(s): T. D. Bradshaw, M.F. G. Stevens and A. D. Westwell

Affiliation:

Abstract: The development of a series of potent and selective antitumour agents, the 2-(4- aminophenyl)benzothiazoles, is described. The original lead compound in this series, CJM 126, exhibits nanomolar in vitro activity against certain human breast cancer cell lines. Structure-activity relationship studies within this simple antitumour benzothiazole pharmacophore revealed that 2-(4-aminophenyl) benzothiazoles bearing a 3- methyl, 3-bromo, 3-iodo or 3-chloro substituent are especially potent, extending the spectrum of in vitro antitumour activity to ovarian, lung, renal and colon carcinoma cell lines with a remarkable selectivity profile (NCI analysis). Other interesting features of this series include the highly unusual transient biphasic dose response relationship and possible unique mechanism of action (NCI COMPARE analysis). 2-(4-Amino-3-methylphenyl)benzothiazole (DF 203) has been selected as the lead compound in this series on the basis of superior in vivo results.

Cite this article as:

Bradshaw D. T., Stevens G. M.F. and Westwell D. A., 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) . https://dx.doi.org/10.2174/0929867013373714