通过碳-氢键硼化反应合成的星形孢菌素类似物。
Staurosporine Analogs Via C-H Borylation.
作者信息
Gayler Kevin M, Kong Ke, Reisenauer Keighley, Taube Joseph H, Wood John L
机构信息
Department of Chemistry and Biochemistry, Baylor University, Waco, Texas 76798, United States.
Department of Biology, Baylor University, Waco, Texas 76798, United States.
出版信息
ACS Med Chem Lett. 2020 Oct 30;11(12):2441-2445. doi: 10.1021/acsmedchemlett.0c00420. eCollection 2020 Dec 10.
Abstract
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.
摘要
星孢菌素是迄今为止分离出的最有效的天然激酶抑制剂之一，并且在多个治疗领域的众多药物开发工作中作为先导化合物。在此我们报告，C-H硼化化学为星孢菌素的类似物提供了获取途径，而这些类似物是过去四十年来制备了1000多种半合成星孢菌素类似物的药物化学家以前无法获得的。
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