Literature DB >> 26793989

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

Marc Perez1, Tahar Ayad1, Philippe Maillos2, Valérie Poughon3, Jacques Fahy4, Virginie Ratovelomanana-Vidal5.   

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.
Copyright © 2016 Elsevier Masson SAS. All rights reserved.

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Keywords:  Anticancer activity; Heck reaction; Plasmatic stability; Securinine; Semisynthesis

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Year:  2016        PMID: 26793989     DOI: 10.1016/j.ejmech.2016.01.007

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  1 in total

1.  Synthesis and Antiproliferative and Metabolic Evaluations of Novel Securinine Derivatives.

Authors:  Marc Perez; Tahar Ayad; Philippe Maillos; Valérie Poughon; Jacques Fahy; Virginie Ratovelomanana-Vidal
Journal:  ACS Med Chem Lett       Date:  2016-02-02       Impact factor: 4.345

  1 in total

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