2. Academic Validation
  3. Isocombretastatins a versus combretastatins a: the forgotten isoCA-4 isomer as a highly promising cytotoxic and antitubulin agent

Isocombretastatins a versus combretastatins a: the forgotten isoCA-4 isomer as a highly promising cytotoxic and antitubulin agent

  • J Med Chem. 2009 Jul 23;52(14):4538-42. doi: 10.1021/jm900321u.
Samir Messaoudi 1,  Bret Tréguier,  Abdallah Hamze,  Olivier Provot,  Jean-François Peyrat,  Jordi Rodrigo De Losada,  Jian-Miao Liu,  Jérôme Bignon,  Joanna Wdzieczak-Bakala,  Sylviane Thoret,  Joëlle Dubois,  Jean-Daniel Brion,  Mouâd Alami
Affiliations

Affiliation

  • 1 Laboratoire de Chimie Therapeutique, Faculte de Pharmacie, Univ Paris-Sud, CNRS, BioCIS-UMR 8076, Clement, Chatenay-Malabry F-92296, France.
PMID: 19530698 DOI: 10.1021/jm900321u
Abstract

Herein is reported a convergent synthesis of isocombretastatins A, a novel class of potent antitubulin agents. These compounds having a 1,1-diarylethylene scaffold constitute the simplest isomers of natural Z-combretastatins A that are easy to synthesize without need to control the Z-olefin geometry. The discovery of isoCA-4 with biological activities comparable to that of CA-4 represents a major progress in this field.

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