N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety ?

Authors: Fortin, SébastienMoreau, Emmanuel; Lacroix, Jacques; Teulade, Jean-Claude; Patenaude, AlexandreC. Gaudreault, René
Abstract: A series of novel N-phenyl-N'-(2-chloroethyl)urea derivatives potentially mimicking the structure of combretastatin A-4 were synthesized and tested for their cell growth inhibition and their binding to the colchicine-binding site of beta-tubulin. Compounds 2a, 3a, and 3b were found to inhibit cell growth at the micromolar level on four human tumor cell lines. Flow cytometric analysis indicates that the new compounds act as antimitotics and arrest the cell cycle in G(2)/M phase. Covalent binding of 2a, 3a, and 3b to the colchicine-binding site of beta-tubulin was confirmed also using SDS-PAGE and competition assays.
Document Type: Article de recherche
Issue Date: 19 January 2007
Open Access Date: 24 April 2019
Document version: AM
Permalink: http://hdl.handle.net/20.500.11794/34534
This document was published in: Bioorganic and medicinal chemistry letters, Vol. 17 (7); 2000-2004 (2007)
Alternative version: 10.1016/j.bmcl.2007.01.023
Collection:Articles publiés dans des revues avec comité de lecture

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