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ID: ALA1132813

Journal: Bioorg Med Chem Lett

Title: Design, synthesis and cytotoxic activities of naphthyl analogues of combretastatin A-4.

Authors: Maya AB, del Rey B, Lamamie de Clairac RP, Caballero E, Barasoain I, Andreu JM, Medarde M.

Abstract: The 3,4,5-trimethoxyphenyl and 3-hydroxy-4-methoxyphenyl rings of combretastatin A-4 are deemed optimal for its activity as antimitotic agent. The replacement of either one by a naphthalene ring results in compounds with a potency comparable to that of the parent compound. These results show that the naphthalene ring is a good surrogate for the 3,4,5-trimethoxyphenyl or the 3-hydroxy-4-methoxyphenyl rings of combretastatin A-4 and that neither of them is essential for the antitumor activity.

CiteXplore: 11086727

DOI: 10.1016/s0960-894x(00)00506-0