Conformationally restricted macrocyclic analogues of combretastatins |
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Authors: | Mateo Carmen Alvarez Raquel Pérez-Melero Concepción Peláez Rafael Medarde Manuel |
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Institution: | Laboratorio de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad de Salamanca, Campus Miguel de Unamuno, Salamanca, Spain. |
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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. |
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