Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373249 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
New analogues of combretastatins have been evaluated as inhibitors of tubulin polymerization. These compounds present a macrocyclic structure, in which the para positions of the aromatic moieties have been linked by a 5- or 6-atoms chain, in order to produce a conformational restriction. This could contribute to determine the active conformation for these ligands. Such a conformational restriction and/or the steric hindrance makes them less potent inhibitors than the model compound CA-4.
Graphical abstractThe activity as inhibitors of tubulin polymerization of macrocyclic analogues of combretastatins is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Carmen Mateo, Raquel Álvarez, Concepción Pérez-Melero, Rafael Peláez, Manuel Medarde,