Novel Imidazole-based Combretastatin A-4 Analogues: Evaluation of Their in Vitro Antitumor Activity and Molecular Modeling Study of Their Binding to the Colchicine Site of Tubulin

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2006 Sep 5

PMID 16950621

Citations 12

Authors

Fabio Bellina

Silvia Cauteruccio

Susanna Monti

Renzo Rossi

Affiliations

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Abstract

The in vitro antitumor activity of novel combretastatin-like 1,5- and 1,2-diaryl-1H-imidazoles was evaluated against the NCI 60 human tumor cell lines panel. Compounds 2d and 2g proved to be more cytotoxic than CA-4 in tests involving their evaluation over a 10(-4)-10(-8) range. Docking experiments showed a good correlation between the MG_MID Log GI(50) values of all these compounds and their calculated interaction energies with the colchicine binding site of alphabeta-tubulin.

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