一系列新戊酰化香豆素类似物的文库。
A library of noviosylated coumarin analogues.
作者信息
Huang Yung-Tzung, Blagg Brian S J
机构信息
Department of Medicinal Chemistry and The Center for Chemical Methodologies and Library Development, The University of Kansas, 1251 Wescoe Hall Drive, Malott Hall 4070, Lawrence, Kansas 66045-7563, USA.
出版信息
J Org Chem. 2007 May 11;72(10):3609-13. doi: 10.1021/jo062083t. Epub 2007 Mar 1.
The DNA gyrase inhibitor, novobiocin, was recently shown to inhibit Hsp90 via a previously unrecognized C-terminal ATP-binding site. Previous structure-activity relationship studies identified key moieties that appear important for Hsp90 inhibitory activity. In an effort to provide a more efficacious lead compound, a parallel library of noviosylated coumarin analogues was prepared.
DNA促旋酶抑制剂新生霉素最近被证明可通过一个先前未被识别的C端ATP结合位点抑制热休克蛋白90（Hsp90）。先前的构效关系研究确定了对Hsp90抑制活性似乎很重要的关键部分。为了提供一种更有效的先导化合物，制备了一个新生霉素化香豆素类似物的平行文库。
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