2. Academic Validation
  3. Synthesis and Antiproliferative and Metabolic Evaluations of Novel Securinine Derivatives

Synthesis and Antiproliferative and Metabolic Evaluations of Novel Securinine Derivatives

  • ACS Med Chem Lett. 2016 Feb 2;7(4):403-7. doi: 10.1021/acsmedchemlett.5b00441.
Marc Perez 1,  Tahar Ayad 1,  Philippe Maillos 2,  Valérie Poughon 3,  Jacques Fahy 3,  Virginie Ratovelomanana-Vidal 1
Affiliations

Affiliations

  • 1 PSL Research University, Chimie ParisTech - CNRS, Institut de Recherche de Chimie Paris , 75005 Paris, France.
  • 2 Institut de Recherche Pierre Fabre , 81600 Gaillac, France.
  • 3 Unité de Service et de Recherche CNRS-Pierre Fabre n°3388 ETaC CRDPF , 31035 Toulouse, France.
PMID: 27096049 DOI: 10.1021/acsmedchemlett.5b00441
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.

Keywords

Securinine; cytotoxicity; semisynthesis.

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