Menzella HG, Tran TT, Carney JR, Lau-Wee J, Galazzo J, Reeves CD, Carreras C, Mukadam S, Eng S, Zhong Z, Timmermans PB, Murli S, Ashley GW
Potent Non-Benzoquinone Ansamycin Heat Shock Protein 90 Inhibitors from Genetic Engineering of Streptomyces hygroscopicus. [JOURNAL ARTICLE]
J Med Chem 2009 Feb 20.
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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