A new family of quinoline and quinoxaline analogues of combretastatins |
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Authors: | Pérez-Melero Concepción Maya Ana B S del Rey Benedicto Peláez Rafael Caballero Esther Medarde Manuel |
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Affiliation: | Laboratorio de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad de Salamanca, Campus Miguel de Unamuno, 37007 Salamanca, Spain. |
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Abstract: | The 3-hydroxy-4-methoxyphenyl ring of combretastatin A-4 can be replaced by a 2-naphthyl moiety without significant loss of cytotoxicity and inhibition of tubulin polymerization potency. In this paper we show that the 6- or 7-quinolyl systems can in turn replace both cyclic moieties, keeping in the first case most of the potency as cytotoxic agent and in the second case as inhibitor of tubulin polymerization, related to the activities displayed by model compounds. |
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