Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 7, Pages 2495-2498Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.01.128
Keywords
hsp90; novobiocin; coumarin inhibitors; anti-tumour; steroid receptors
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A new series of coumarin inhibitors of hsp90 lacking the noviose moiety as well as substituents on C-7 and C-8 positions of the aromatic ring was synthesised and their hsp90 inhibitory activity has been delineated: for example, their capacity to induce the degradation of client proteins and to inhibit estradiol-induced transcription in human breast cancer cells. In cell proliferation assay, the most active compound 5g was similar to 8 times more potent than the parent novobiocin natural compound. (C) 2008 Elsevier Ltd. All rights reserved.
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