TOPOISOMERASE-II INHIBITORS - SYNTHETIC HYBRIDIZATION OF 4-QUINOLONESAND ANTHRACYCLINES

Authors
KULKARNI T MITSCHER LA SHEN LL TELIKEPALLI H WEI D
Citation
T. Kulkarni et al., TOPOISOMERASE-II INHIBITORS - SYNTHETIC HYBRIDIZATION OF 4-QUINOLONESAND ANTHRACYCLINES, Bioorganic & medicinal chemistry letters, 7(9), 1997, pp. 1097-1100
Citations number
16
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
9
Year of publication
1997
Pages
1097 - 1100
Database
ISI
SICI code
0960-894X(1997)7:9<1097:TI-SHO>2.0.ZU;2-X
Abstract
A series of hybrid molecules (14-16) combining certain structural feat ures of both 4-quinolone antimicrobial inhibitors of DNA gyrase and an thracycline inhibitors of mammalian topoisomerase II were prepared syn thetically in six chemical steps from digiferrol dimethyl ether(3). Th e resulting hybrids were, unfortunately, inactive against both bacteri a and mammalian cells as well as purified topoisomerases at doses wher e ciprofloxacin and doxorubicin are highly active. (C) 1997 Elsevier S cience Ltd.