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

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

Journal Name: Current Medicinal Chemistry

Volume 8 , Issue 2 , 2001

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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.

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Article Details

Year: 2001
Published on: 01 March, 2012
Page: [203 - 210]
Pages: 8
DOI: 10.2174/0929867013373714
Price: $65

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