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.

Graphical abstractA series of 4′-aminochalcone-based maleimides were identified as novel cytostatic agents against three representative cancer cell lines. Representative compounds were well tolerated by mice in in vivo survival and toxicity studies.Figure optionsDownload full-size imageDownload as PowerPoint slide