Synthesis and Antitumor Activity of Diosgenin Hydroxamic Acid and Quaternary Phosphonium Salt Derivatives

Diosgenin, a component separated from Dioscorea plants, is an important starting material for steroid hormone drugs and semisynthetic steroids. In the work, two series of diosgenin derivatives were designed, synthesized, and evaluated for their cellular anticancer activities. Most of the target compounds exhibited good inhibitory activities against four cell lines, Aspc-1 (human and SW620 (human metastatic pancreatic cancer cells). Among them, the representative compound 2.2f exhibited 7.9-341.7-fold antiproliferative activities against the above-mentioned four cell lines compared with the lead compound diosgenin.

Automated summary

In this study, two series of diosgenin derivatives were synthesized and evaluated for their cellular anticancer activities. The representative compound 2.2f exhibited significantly higher antiproliferative activities against four cell lines compared with the lead compound diosgenin.