海幔二酮类似物的合成及其对 CHK1 的抑制活性。
Synthesis and CHK1 inhibitory potency of Hymenialdisine analogues.
机构信息
Medicinal Chemistry Division D, Institut de Recherche Servier, 11 rue des Moulineaux, 92150 Suresnes, France.
出版信息
Bioorg Med Chem Lett. 2009 Feb 1;19(3):841-4. doi: 10.1016/j.bmcl.2008.12.001. Epub 2008 Dec 7.
PMID:19111462
Abstract
A series of thieno[3,2-b]pyrroloazepinones derivatives related to Hymenialdisine were prepared and tested for CHK1 inhibitory activity. Nanomolar inhibitions were achieved when electron-withdrawing substituents were introduced at position 3 of the thiophene ring.
摘要
一系列与海鞘素有关的噻吩并[3,2-b]吡咯并氮杂卓衍生物被制备并测试了对 CHK1 的抑制活性。当在噻吩环的 3 位引入吸电子取代基时，可达到纳摩尔级的抑制。
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