Structure Activity Relationship of 4-Phenyl-1-(1-Acylindolin-5-Ylsulfonyl)Pyrrolidin-2-Ones on Anticancer Activity

Microtubules play a dynamic role during cell division. In our early studies 4-phenyl-1-(1-acylindoline-5-sulfonylimidazolones were thoroughly explored and found that the indoline bicyclic system next to the sulfonyl group is very important for cytotoxicity. In this research, imidazolone motif was replaced with pyrrolidin-2-one and this isosteric replacement led to show some promising activity. Thus, the structure activity relationship of 4-phenyl-1-(1-acylindolin-5-ylsulfonyl)pyrrolidin-2-ones with the various acyl group at the indoline NH was explored. The presence of benzoyl groups with electron donating group was the more favorable for cytotoxicity while less bulky alkanoyl groups led to decrease cytotoxicity.