Design, synthesis and biological evaluation of novel steroidal spiro-oxindoles as potent antiproliferative agents.

Highlights: [•] Two series of novel steroidal spiro-oxindoles were efficiently synthesized. [•] Most of these compounds exhibited broad-spectrum antiproliferative activities. [•] Some of them were more potent than 5-Fu against four human cancer cell lines. [•] Compound 3g showed good antiproliferative activity against SMMC-7721 (IC50 =0.71μM). [•] Compound 3n showed cell cycle arrest at G2/M phase and induced early apoptosis. [Copyright &y& Elsevier]