Title: Cytostatic activity of novel 4'-aminochalcone-based imides
Authors: Jha, Amitabh ×
Mukherjee, Chandrani
Rolle, Alfred J
De Clercq, Erik
Balzarini, Jan
Stables, James P #
Issue Date: Aug-2007
Publisher: Pergamon Press
Series Title: Bioorganic & Medicinal Chemistry Letters vol:17 issue:16 pages:4545-4550
Abstract: A series of nine 1-(4-((E)-3-arylacryloyl)phenyl)-1H-pyrrole-2,5-diones 3a-i (4'-aminochalcone-based maleimides) was synthesized as candidate cytotoxic agents. The efficacy of these potential cytotoxics were evaluated against three representative cell lines and more than half of the drug candidates proved to exhibit significant cytostatic activity in vitro. QSAR studies using statistical analyses on several physicochemical parameters and IC50 values resulted in a few very important correlations which will aid in later the amplification of the project. Representative test compounds were well tolerated by mice in in vivo survival and toxicity studies.
ISSN: 0960-894X
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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