3-BENZYL-QUINOLONES - NOVEL, POTENT INHIBITORS OF MAMMALIAN TOPOISOMERASE-II

Authors
EISSENSTAT MA KUO GH WEAVER JD WENTLAND MP ROBINSON RG KLINGBEIL KM DANZ DW CORBETT TH COUGHLIN SA
Citation
Ma. Eissenstat et al., 3-BENZYL-QUINOLONES - NOVEL, POTENT INHIBITORS OF MAMMALIAN TOPOISOMERASE-II, Bioorganic & medicinal chemistry letters, 5(9), 1995, pp. 1021-1026
Citations number
7
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
9
Year of publication
1995
Pages
1021 - 1026
Database
ISI
SICI code
0960-894X(1995)5:9<1021:3-NPIO>2.0.ZU;2-S
Abstract
Replacement of the 3-carboxy group of quinolone topoisomerase II inhib itors by hydroxy substituted benzyl groups resulted in potent topoisom erase 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 a s murine antitumor activity.