Potent Non-Benzoquinone Ansamycin Heat Shock Protein 90 Inhibitors from Genetic Engineering of Streptomyces hygroscopicus
Journal of Medicinal Chemistry2009Vol. 52(6), pp. 1518–1521
Citations Over TimeTop 15% of 2009 papers
Hugo G. Menzella, Thomas-Toan Tran, John R. Carney, Janice Lau-Wee, Jorge L. Galazzo, Christopher D. Reeves, Christopher W. Carreras, Sophie Mukadam, Sara Eng, Ziyang Zhong, Pieter B.M.W.M. Timmermans, Sumati Murli, Gary W. Ashley
Abstract
Inhibition of the protein chaperone Hsp90 is a promising new approach to cancer therapy. We describe the preparation of potent non-benzoquinone ansamycins. One of these analogues, generated by feeding 3-amino-5-chlorobenzoic acid to a genetically engineered strain of Streptomyces hygroscopicus, shows high accumulation and long residence time in tumor tissue, is well-tolerated upon intravenous dosing, and is highly efficacious in the COLO205 mouse tumor xenograft model.
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