Alkylide derivatives of diphyllin: synthesis and preliminary anticancer evaluation

Abstract

Fourteen diphyllin 4-C-substituted alkylide derivatives were designed and synthesized using a Heck coupling and subsequent hydrogenation reaction. Olefins 3g and 3i exhibited the highest cytotoxicity on breast cancer cell lines MCF-7 with IC₅₀ values of 0.08 and 0.07 µM, and they showed weaker V-ATPase inhibitory potency compared to diphyllin.

Keywords:

• Diphyllin
• alkylide derivatives
• synthesis
• anticancer agents

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

The authors are grateful for financial support provided by Shanghai Rulink Biopharmaceutical Corporation (Grant number 22ZH043).