A library of noviosylated coumarin analogues
A library of noviosylated coumarin analogues
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DOI：
10.1021/jo062083t
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发表时间：
2007-05-11
影响因子：
3.6
通讯作者：
Blagg, Brian S. J.
中科院分区：
文献类型：
--
作者：
Huang, Yung-Tzung;Blagg, Brian S. J.
DNA促旋酶抑制剂新生霉素（novobiocin）最近被证明可以通过以前未被识别的C-末端ATP结合位点抑制Hsp 90。先前的结构-活性关系研究确定了对Hsp 90抑制活性重要的关键部分。为了提供更有效的先导化合物，制备了Noviosylated香豆素类似物的平行文库。
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.