Conformationally restricted macrocyclic analogues of combretastatins.
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.
Mateo
Carmen
C
Laboratorio de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad de Salamanca, Campus Miguel de Unamuno, Salamanca, Spain.
Alvarez
Raquel
R
Pérez-Melero
Concepción
C
Peláez
Rafael
R
Medarde
Manuel
M
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*
D001632:Bibenzyls; D047028:Macrocyclic Compounds; D013267:Stilbenes; D014404:Tubulin; D050257:Tubulin Modulators; C040105:combretastatin