Jump to main content
Jump to site search
Access to RSC content Close the message box

Continue to access RSC content when you are not at your institution. Follow our step-by-step guide.


Issue 10, 2015
Previous Article Next Article

Synthesis and evaluation of hybrid molecules targeting the vinca domain of tubulin

Author affiliations

Abstract

Some hybrids of vinca alkaloids and phomopsin A, linked by a glycine pattern, have been synthesized in one or two steps, by an insertion reaction and shown to inhibit microtubule assembly. These compounds have been elaborated in order to interact with both the “vinca site” and the “peptide site” of the vinca domain in tubulin. Two out of three hybrids are potent inhibitors of microtubules assembly and they present good cytotoxicity against different cell lines. Molecular modelling studies show that they could bind, within the vinca domain, in similar spatial regions as those of vinca and phomopsin thanks to the flexibility provided by the glycine linker used to elaborate these hybrids.

Graphical abstract: Synthesis and evaluation of hybrid molecules targeting the vinca domain of tubulin

Back to tab navigation

Supplementary files

Article information


Submitted
03 Oct 2014
Accepted
19 Jan 2015
First published
20 Jan 2015

Org. Biomol. Chem., 2015,13, 3144-3154
Article type
Paper
Author version available

Synthesis and evaluation of hybrid molecules targeting the vinca domain of tubulin

O. Gherbovet, P. A. Sánchez-Murcia, M. C. García Alvarez, J. Bignon, S. Thoret, F. Gago and F. Roussi, Org. Biomol. Chem., 2015, 13, 3144
DOI: 10.1039/C4OB02114B

Social activity

Search articles by author

Spotlight

Advertisements