Antitumor benzothiazoles. 3. 1 Synthesis of 2-(4-aminophenyl) benzothiazoles and evaluation of their activities against breast cancer cell lines in vitro and in vivo

…, P Lelieveld, I Fichtner, MFG Stevens

Index: Shi, Dong-Fang; Bradshaw, Tracey D.; Wrigley, Samantha; McCall, Carol J.; Lelieveld, Peter; Fichtner, Iduna; Stevens, Malcolm F. G. Journal of Medicinal Chemistry, 1996 , vol. 39, # 17 p. 3375 - 3384

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Citation Number: 346

Abstract

A new series of 2-(4-aminophenyl) benzothiazoles substituted in the phenyl ring and benzothiazole moiety has been synthesized by simple, high-yielding routes. The parent molecule 5a shows potent inhibitory activity in vitro in the nanomolar range against a panel of human breast cancer cell lines, but is inactive (IC50> 30 μM) against other cell types: activity against the sensitive breast lines MCF-7 and MDA 468 is characterized by a ...