Staurosporine Analogs Via C–H Borylation
Staurosporine Analogs Via C–H Borylation
复制标题
通过 C–H 硼化获得星形孢菌素类似物
DOI：
10.1021/acsmedchemlett.0c00420
复制
发表时间：
2020
影响因子：
4.2
通讯作者：
Wood, John L.
中科院分区：
文献类型：
--
作者：
Gayler, Kevin M.;Kong, Ke;Reisenauer, Keighley;Taube, Joseph H.;Wood, John L.
星状孢子素是迄今为止分离出来的最有效的自然发生的激酶抑制剂之一，并已在几个治疗领域作为许多药物开发努力的先导化合物。在此，我们报告了C-H硼化化学提供了获得以前药物化学家无法获得的星孢菌素类似物的途径，在过去的40年中，他们已经制备了1000多个半合成星孢菌素类似物。
Staurosporine is among the most potent naturally occurring kinase inhibitors isolated to date and has served as a lead compound for numerous drug development efforts in several therapeutic areas. Herein we report that C–H borylation chemistry provides access to analogs of staurosporine that were previously inaccessible to medicinal chemists who, in the past four decades, have prepared over 1000 semisynthetic staurosporine analogs.