2. Academic Validation
  3. Synthesis and biological evaluation of novel heterocyclic derivatives of combretastatin A-4

Synthesis and biological evaluation of novel heterocyclic derivatives of combretastatin A-4

  • Bioorg Med Chem Lett. 2012 Dec 1;22(23):7227-31. doi: 10.1016/j.bmcl.2012.09.047.
Thi Thanh Binh Nguyen 1,  Thierry Lomberget,  Ngoc Chau Tran,  Evelyne Colomb,  Lore Nachtergaele,  Sylviane Thoret,  Joëlle Dubois,  Joren Guillaume,  Rawad Abdayem,  Marek Haftek,  Roland Barret
Affiliations

Affiliation

  • 1 Université de Lyon, Université Lyon 1, Faculté de Pharmacie, ISPB, EA 4446 Biomolécules, Cancer et Chimiorésistances, SFR Santé Lyon-Est CNRS UMS3453-INSERM US7, 8 avenue Rockefeller, F-69373 Lyon cedex 08, France.
PMID: 23063401 DOI: 10.1016/j.bmcl.2012.09.047
Abstract

A novel series of combretastatin A-4 heterocyclic analogues was prepared by replacement of the B ring with indole, benzofurane or benzothiophene, attached at the C2 position. These compounds were evaluated for their abilities to inhibit tubulin assembly: derivative cis3b, having a benzothiophene, showed an activity similar to those of colchicine or deoxypodophyllotoxine. The antiproliferative and antimitotic properties of cis3b against keratinocyte Cancer cell lines were also evaluated and the intracellular organization of microtubules in the cells after treatment with both stereoisomers of 3b was also determined, using confocal microscopy.

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