Antitumor agents. Part 186:11For part 185, see ref. [1]. Synthesis and biological evaluation of demethylcolchiceinamide analogues as cytotoxic DNA topoisomerase II inhibitors
作者： Jian Guan , Xiao-Kang Zhu , Yoko Tachibana , Kenneth F. Bastow , Arnold Brossi
DOI: 10.1016/S0968-0896(98)00165-5
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摘要: Demethylation of colchiceinamide (2) and its analogues (3-10) afforded a novel class mammalian DNA topoisomerase II inhibitors (2a-10a) without displaying tubulin inhibitory activity. All target compounds inhibited the catalytic activity at drug concentrations 100 microM. An in vitro cytotoxicity assay indicated that 3a 8a were strong tissue-selective cytotoxic agents against MCF-7 breast cancer cell line (IC50 = 0.36 0.48 microgram/mL, respectively) CAKI-1 renal 0.72 0.96 respectively).
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