Indolocarbazole poisons of human topoisomerase I: Regioisomeric analogues of ED-110

Authors
Zembower, DE Zhang, HP Lineswala, JP Kuffel, MJ Aytes, SA Ames, MM
Citation
De. Zembower et al., Indolocarbazole poisons of human topoisomerase I: Regioisomeric analogues of ED-110, BIOORG MED, 9(2), 1999, pp. 145-150
Citations number
16
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
2
Year of publication
1999
Pages
145 - 150
Database
ISI
SICI code
0960-894X(19990118)9:2<145:IPOHTI>2.0.ZU;2-6
Abstract
All four "symmetrical" regioisomers of ED-110, an indolocarbazole derivativ e having potent activity against human topoisomerase I (Topo I) were synthe sized. The isomer containing hydroxyl groups in the 3- and 9-positions was approximately ten-fold more active against Topo I, and 5- to 35-fold more a ctive against human solid tumor cell lines in vitro, relative to ED-110. (C ) 1999 Elsevier Science Ltd. All rights reserved.