2. Academic Validation
  3. Synthesis and biological evaluation of new securinine analogues as potential anticancer agents

Synthesis and biological evaluation of new securinine analogues as potential anticancer agents

  • Eur J Med Chem. 2016 Feb 15:109:287-93. doi: 10.1016/j.ejmech.2016.01.007.
Marc Perez 1,  Tahar Ayad 1,  Philippe Maillos 2,  Valérie Poughon 3,  Jacques Fahy 4,  Virginie Ratovelomanana-Vidal 5
Affiliations

Affiliations

  • 1 PSL Research University, Chimie ParisTech - CNRS, Institut de Recherche de Chimie Paris, Paris, 75005, France.
  • 2 Institut de Recherche Pierre Fabre, Gaillac, 81600, France.
  • 3 Unité de Service et de Recherche CNRS-Pierre Fabre n°3388 ETaC CRDPF, Toulouse, 31035, France.
  • 4 Unité de Service et de Recherche CNRS-Pierre Fabre n°3388 ETaC CRDPF, Toulouse, 31035, France. Electronic address: jacques.fahy@pierre-fabre.com.
  • 5 PSL Research University, Chimie ParisTech - CNRS, Institut de Recherche de Chimie Paris, Paris, 75005, France. Electronic address: virginie.vidal@chimie-paristech.fr.
PMID: 26793989 DOI: 10.1016/j.ejmech.2016.01.007
Abstract

A series of new securinine analogues was prepared by Heck reaction from readily accessible securinine and commercially available iodoarenes. The in vitro cytotoxicity of the prepared compounds was assayed against a panel of four Cancer cell lines: A375, A549, HCT-116 and HL-60 showing promising growth inhibition with excellent IC50 values in the nanomolar range. The plasmatic stability of the most potent analogue was also investigated demonstrating that they might serve as valuable leads for the development of Anticancer drugs.

Keywords

Anticancer activity; Heck reaction; Plasmatic stability; Securinine; Semisynthesis.

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