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
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.