Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1365217 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
Abstract
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.
Graphical abstractThe synthesis and biological activity of a new series of denoviose-coumarins related to novobiocin are described.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Christine Radanyi, Gaëlle Le Bras, Samir Messaoudi, Céline Bouclier, Jean-François Peyrat, Jean-Daniel Brion, Véronique Marsaud, Jack-Michel Renoir, Mouâd Alami,