Synthesis, DNA binding, topoisomerases inhibition and cytotoxic propertiesof 4-arylcarboxamidopyrrolo-2-carboxyanilides

Authors
Dudouit, F Goossens, JF Houssin, R Henichart, JP Colson, P Houssier, C Gelus, N Bailly, C
Citation
F. Dudouit et al., Synthesis, DNA binding, topoisomerases inhibition and cytotoxic propertiesof 4-arylcarboxamidopyrrolo-2-carboxyanilides, BIOORG MED, 10(6), 2000, pp. 553-557
Citations number
22
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
6
Year of publication
2000
Pages
553 - 557
Database
ISI
SICI code
0960-894X(20000320)10:6<553:SDBTIA>2.0.ZU;2-T
Abstract
Three 4-arylcarboxamidopyrrolo-2-carboxyanilides bearing different substitu ents on the pyrrole nitrogen were synthesized and evaluated for their capac ities to bind to specific sequences within the minor groove of DNA and to i nhibit human topoisomerases I and II in vitro. The cytotoxicity of the drug s correlates with their DNA binding affinities. The two drugs bearing a N-m ethyl or N-benzyl pyrrole stabilize topoisomerase I-DNA complexes. (C) 2000 Elsevier Science Ltd. All rights reserved.