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Elaboration of simplified vinca alkaloids and phomopsin hybrids.

Chemical biology & drug design (2010-07-28)
Quoc Anh Ngo, Fanny Roussi, Sylviane Thoret, Françoise Guéritte
ABSTRACT

Nine simplified vinca alkaloids and phomospin A hybrids, in which vindoline moiety has been replaced by a simpler scaffold, have been elaborated to evaluate their activity on the inhibition of tubulin polymerization. This article deals with the synthesis of various simplified vinca alkaloids, using a stereoselective coupling of catharantine with reactive aromatic compounds and methanol as well as their subsequent condensation with a large peptide chain mimicking those of phomopsin A. Biological evaluation and molecular modeling studies are also reported.