Synthesis and Antiproliferative and Metabolic Evaluations of Novel Securinine Derivatives

详细信息    查看全文

• 作者：Marc Perez ; Tahar Ayad ; Philippe Maillos ; Valérie Poughon ; Jacques Fahy ; Virginie Ratovelomanana-Vidal
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：April 14, 2016
• 年：2016
• 卷：7
• 期：4
• 页码：403-407
• 全文大小：461K
• 年卷期：0
• ISSN：1948-5875

文摘

New securinine analogues have been prepared by semisynthesis. Two series were developed using either Suzuki or Sonogashira cross coupling reactions. The in vitro cytotoxicity of the compounds was assayed against HCT-116 colon cancer cells. The most potent derivatives showed promising growth inhibition on four tumoral cell lines giving a valuable insight on the structure–activity relationship (SAR) of securinine. Moreover, high antiproliferative effect against A-375 (melanoma) was observed with IC₅₀ up to 60 nM.