Multicomponent assembly of novel antiproliferative steroidal dihydropyridinyl spirooxindoles

作者：Zhang, Yan-Ling; Li, Ya-Fei; Wang, Jun-Wei; Yu, Bin; Shi, Yun-Kai; Liu, Hong-Min^*

来源：Steroids, 2016, 109: 22-28.

DOI：10.1016/j.steroids.2016.03.005

• Multicomponent assembly
• Spirooxindoles
• Dihydropyridine
• Cytotoxicity

Multicomponent assembly of steroidal dihydropyridinyl spirooxindoles from pregnenolone, isatins, malononitrile, and ammonium acetate is described, which involves the formation of two C-C bonds, two C-N bonds, and an all-carbon quaternary stereogenic center in a single operation. MIT assays showed that some of these compounds had moderate to excellent cytotoxicity against the tested cancer cell lines and were more potent than 5-FU. Particularly, compound 5o represented excellent inhibitory effect toward EC-109 (IC50 = 0.3 mu M), being about 33-fold more potent than 5-FU.

• 出版日期2016-5
• 单位许昌学院; 郑州大学