RELATIONSHIP OF STRUCTURE OF BRIDGED (2,6-DIMETHYL-4-PYRIDINYL)-QUINOLONES TO MAMMALIAN TOPOISOMERASE-II INHIBITION

Authors
WENTLAND MP LESHER GY REUMAN M PILLING GM SAINDANE MT PERNI RB EISSENSTAT MA WEAVER JD SINGH B RAKE J COUGHLIN SA
Citation
Mp. Wentland et al., RELATIONSHIP OF STRUCTURE OF BRIDGED (2,6-DIMETHYL-4-PYRIDINYL)-QUINOLONES TO MAMMALIAN TOPOISOMERASE-II INHIBITION, Bioorganic & medicinal chemistry letters, 3(8), 1993, pp. 1711-1716
Citations number
21
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
8
Year of publication
1993
Pages
1711 - 1716
Database
ISI
SICI code
0960-894X(1993)3:8<1711:ROSOB(>2.0.ZU;2-K
Abstract
Several enantiomerically pure (2,6-dimethyl-4-pyridinyl)quinolones, pr eviously shown to be potent inhibitors of bacterial DNA gyrase, exhibi t topoisomerase II inhibitory activity. Among these and other analogue s, topoisomerase II inhibitory potency was found to be a sensitive fun ction of the size and substitution of the bridge spanning the 1- and 8 -positions of the quinoline ring. The 6-fluoro group was required for activity.