title: Conformationally restricted macrocyclic analogues of combretastatins.
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.
authors: Laboratorio de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad de Salamanca, Campus Miguel de Unamuno, Salamanca, Spain.
authors: Carmen
authors: C
authors: Mateo
authors: Raquel
authors: R
authors: Alvarez
authors: Concepción
authors: C
authors: Pérez-Melero
authors: Rafael
authors: R
authors: Peláez
authors: Manuel
authors: M
authors: Medarde
mesh_terms: D001632:Bibenzyls / Q000737:chemistry* / Q000494:pharmacology; D047028:Macrocyclic Compounds / Q000737:chemistry* / Q000494:pharmacology; D008958:Models, Molecular; D008968:Molecular Conformation; D013267:Stilbenes / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014404:Tubulin / Q000737:chemistry* / Q000187:drug effects; D050257:Tubulin Modulators / Q000737:chemistry*
chemical_list: D001632:Bibenzyls; D047028:Macrocyclic Compounds; D013267:Stilbenes; D014404:Tubulin; D050257:Tubulin Modulators; C040105:combretastatin