మెడిసినల్ కెమిస్ట్రీ

Synthesis and Anti-Cancer Evaluation of Spiro-indolinone Derivatives

Abstract

Liang Hong, Jie Tong, Guangliang Yu and Chunqi Hu

A series of spiro-indolin-2-one derivatives were designed and synthesized as p53-MDM2 binding inhibitors. Though p53-MDM2 binding inhibitory and activities against p53 wild-type cell lines of most compounds were not that promising, some obtained structures showed moderate to strong inhibitory activities (IC50<0.08 μM) against p53 mutant cell lines (SW620), suggesting that these compounds may have different modes of action to p53 pathway, further studies on treatment of p53 mutant tumors are under investigation.cc