Synthesis and biological activity of simplified denoviose-coumarins related to novobiocin as potent inhibitors of heat-shock protein 90 (hsp90)
The synthesis and biological activity of a new series of denoviose-coumarins related to novobiocin are described. 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 a...
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Published in | Bioorganic & medicinal chemistry Vol. 18; no. 7; pp. 2495 - 2498 |
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Main Authors | , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
Oxford
Elsevier Ltd
01.04.2008
Elsevier |
Subjects | |
Online Access | Get full text |
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Summary: | The synthesis and biological activity of a new series of denoviose-coumarins related to novobiocin are described.
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 ∼8 times more potent than the parent novobiocin natural compound. |
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Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 0960-894X 0968-0896 1464-3405 1464-3391 |
DOI: | 10.1016/j.bmcl.2008.01.128 |