Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 52, Issue 6, Pages 1518-1521Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm900012a
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Funding
- National Institutes of Health [5R44 CA096262-03]
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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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