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Synthesis and Antiproliferative and Metabolic Evaluations of Novel Securinine Derivatives.

ABSTRACT: 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.

SUBMITTER: Perez M 

PROVIDER: S-EPMC4834650 | biostudies-literature | 2016 Apr

REPOSITORIES: biostudies-literature

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Synthesis and Antiproliferative and Metabolic Evaluations of Novel Securinine Derivatives.

Perez Marc M   Ayad Tahar T   Maillos Philippe P   Poughon Valérie V   Fahy Jacques J   Ratovelomanana-Vidal Virginie V  

ACS medicinal chemistry letters 20160202 4

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 I  ...[more]

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