Cytostatic activity of novel 4'-aminochalcone-based imides.
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.
Jha
Amitabh
A
Department of Chemistry, Acadia University, Wolfville, NS, Canada B4P 2R6. ajha@acadiau.ca
Mukherjee
Chandrani
C
Rolle
Alfred J
AJ
De Clercq
Erik
E
Balzarini
Jan
J
Stables
James P
JP
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D002493:Central Nervous System Diseases / Q000139:chemically induced; D047188:Chalcones / Q000737:chemistry* / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D007094:Imides / Q000737:chemistry* / Q000494:pharmacology*; D051379:Mice; D013329:Structure-Activity Relationship; D018675:Toxicity Tests
D000970:Antineoplastic Agents; D047188:Chalcones; D007094:Imides