Synthesis and biological activity of simplified denoviose-coumarins related to novobiocin as potent inhibitors of heat-shock protein 90 (hsp90)
- 作者：Christine Radanyi ; Gaë ; lle Le Bras ; Samir Messaoudi ; Cé ; line Bouclier ; Jean-Franç ; ois Peyrat ; Jean-Daniel Brion ; Vé ; ronique Marsaud ; Jack-Michel Renoir ; Mouâ ; d Alami
- 关键词：hsp90 ; Novobiocin ; Coumarin inhibitors ; Anti-tumour ; Steroid receptors
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2008
- 期刊代码：10_0960894x
- 类别：ch
- 出版时间：1 April 2008
- 卷：18
- 期：7
- 页码：2495-2498
- 文件大小：177 K
摘要
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 
le="not, vert, similar" border="0">8 times more potent than the parent novobiocin natural compound.
le="not, vert, similar" border="0">8 times more potent than the parent novobiocin natural compound.