1. Academic Validation
  2. Synthesis and biological activity of naphthalene analogues of phenstatins: naphthylphenstatins

Synthesis and biological activity of naphthalene analogues of phenstatins: naphthylphenstatins

  • Bioorg Med Chem Lett. 2007 Jun 15;17(12):3417-20. doi: 10.1016/j.bmcl.2007.03.082.
Concepción Alvarez 1 Raquel Alvarez Purificación Corchete Concepción Pérez-Melero Rafael Peláez Manuel Medarde
Affiliations

Affiliation

  • 1 Departament de Química Farmacéutica, Facultad de Farmacia, Universidad de Salamanca, Campus Miguel de Unamuno, 37007 Salamanca, Spain.
Abstract

Novel phenstatin analogues with a 2-naphthyl moiety combined with either a 2,3,4- or a 3,4,5-trimethoxyphenyl ring have been synthesized, and their tubulin polymerization inhibiting and cytotoxic activities have been evaluated. The 2-naphthyl ring is a better replacement for the 3-hydroxy-4-methoxyphenyl ring in the phenstatin series than in the combretastatin series. For the naphthylphenstatins, the carbonyl is required, and the preferred orientation of the trimethoxyphenyl ring is the one found in combretastatins.

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