Combretastatin-like chalcones as inhibitors of microtubule polymerisation. Part 2: Structure-based discovery of alpha-aryl chalcones

…, S Armitage, JFD Chabert, E Bennett, J Nettles…

Index: Ducki, Sylvie; Mackenzie, Grant; Greedy, Ben; Armitage, Simon; Chabert, Jeremie Fournier Dit; Bennett, Elizabeth; Nettles, Jim; Snyder, James P.; Lawrence, Nicholas J. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 22 p. 7711 - 7722

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Citation Number: 60

Abstract

Tubulin is an important molecular target in cancer chemotherapy. Antimitotic agents able to bind to the protein are currently under study, commonly used in the clinic to treat a variety of cancers and/or exploited as probes to investigate the protein's structure and function. Here we report the binding modes for a series of colchicinoids, combretastatin A4 and chalcones established from docking studies carried out on the structure of tubulin in complex with ...