Antitumor agents. Part 186: Synthesis and biological evaluation of demethylcolchiceinamide analogues as cytotoxic DNA topoisomerase II inhibitors

…, Y Tachibana, KF Bastow, A Brossi, E Hamel…

文献索引：Guan, Jian; Zhu, Xiao-Kang; Tachibana, Yoko; Bastow, Kenneth F.; Brossi, Arnold; Hamel, Ernest; Lee, Kuo-Hsiung Bioorganic and Medicinal Chemistry, 1998 , vol. 6, # 11 p. 2127 - 2131

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被引用次数: 6

摘要

Demethylation of colchiceinamide (2) and its analogues (3–10) afforded a novel class of mammalian DNA topoisomerase II inhibitors (2a–10a) without displaying tubulin inhibitory activity. All target compounds inhibited the catalytic activity of topoisomerase II at drug concentrations at 100μM. An in vitro cytotoxicity assay indicated that compounds 3a and 8a were strong and tissue-selective cytotoxic agents against the MCF-7 breast cancer cell ...