title: Cytostatic activity of novel 4'-aminochalcone-based imides.
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.
authors.affiliation: Department of Chemistry, Acadia University, Wolfville, NS, Canada B4P 2R6. ajha@acadiau.ca
authors.forename: Amitabh
authors.initials: A
authors.lastname: Jha
authors.forename: Chandrani
authors.initials: C
authors.lastname: Mukherjee
authors.forename: Alfred J
authors.initials: AJ
authors.lastname: Rolle
authors.forename: Erik
authors.initials: E
authors.lastname: De Clercq
authors.forename: Jan
authors.initials: J
authors.lastname: Balzarini
authors.forename: James P
authors.initials: JP
authors.lastname: Stables
mesh_terms: 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
chemical_list: D000970:Antineoplastic Agents; D047188:Chalcones; D007094:Imides