Spirooxadiazoline oxindoles with promising in vitro antitumor activities

Abstract

This paper reports the synthesis and biological evaluation of thirty one spirooxadiazoline oxindoles as potential anticancer agents. Nine compounds showed an antiproliferative activity below 10 μM, with four compounds more active than the positive control nutlin-3a in HCT 116 p53^(+/+) cell line. Moreover, compound 1aa was shown to induce p53 stabilization and transactivation, to induce apoptosis, and to inhibit the interaction between p53 and MDM2 in a live-cell bimolecular fluorescence complementation assay.