Open AccessStaurosporine Analogs Via C–H Borylation
Author(s) -
Kevin M. Gayler,
Ke Kong,
Keighley Reisenauer,
Joseph H. Taube,
John L. Wood
Publication year - 2020
Publication title -
acs medicinal chemistry letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.065
H-Index - 66
ISSN - 1948-5875
DOI - 10.1021/acsmedchemlett.0c00420
Subject(s) - staurosporine , borylation , chemistry , pharmacology , drug , kinase , medicine , biochemistry , protein kinase c , organic chemistry , alkyl , aryl
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.