Relationship of structure of bridged (2,6-dimethyl-4-pyridinyl)quinolones to mammalian topoisomerase II inhibition

Bioorganic & Medicinal Chemistry Letters
1993.0

Abstract

Several enantiomerically pure (2,6dimethyl-4-pyridinyl)quinolones, previously shown to be potent inhibitors of bacterial DNA gyrase, exhibit topoisomerase II inhibitory activity. Among these and other analogues, topoisomerase II inhibitory potency was found to be a sensitive function of the size and substitution of the bridge spanning the l- and II-positions of the quinoline ring. The 6-fluoro group was requited for activity.

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