3-benzyl-quinolones: Novel, potent inhibitors of mammalian topoisomerase II

Bioorganic & Medicinal Chemistry Letters
1995.0

Abstract

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 EC50 of 96 nM and had potent in vitro cytotoxicity as well as murine antitumor activity.

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