3-Benzyl-Quinolones - Novel, Potent Inhibitors Of Mammalian Topoisomerase-Ii

Michael A. Eissenstat,Gee-Hong Kuo,John D. Weaver,Mark P. Wentland,Ronald G. Robinson,Kristina M. Klingbeil,Deborah W. Danz,Thomas H. Corbett,Susan A. Coughlin

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（1995）

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摘要

Replacement of the 3-carboxy group of quinolone topoisomerase II inhibitors by hydroxy substituted benzyl groups resulted in potent topoisomerase II inhibitors. The 2,6-dihydroxybenzyl analog, Win 64593, had a topo II EC(50) of 96 nM and had potent in vitro cytotoxicity as well as murine antitumor activity.

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