期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 23, 页码 6273-6278出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.09.081
关键词
Dihydroxylphenyl amides; Hsp90; Inhibitor
Information from X-ray crystal structures were used to optimize the potency of a HTS hit in a Hsp90 competitive binding assay. A class of novel and potent small molecule Hsp90 inhibitors were thereby identified. Enantio-pure compounds 31 and 33 were potent in PGA-based competitive binding assay and inhibited proliferation of various human cancer cell lines in vitro, with IC50 values averaging 20 nM. (C) 2008 Elsevier Ltd. All rights reserved.
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