化学
蛋白激酶A
激酶
生物化学
丝裂原活化蛋白激酶激酶
MAP激酶激酶激酶
c-Raf公司
丝裂原活化蛋白激酶
细胞周期蛋白依赖激酶2
小分子
地图2K7
细胞周期蛋白依赖激酶9
MAPK/ERK通路
作者
Songnian Lin,Sunita Malkani,Matthew Lombardo,Lihu Yang,Sander G. Mills,Kevin T. Chapman,James E. Thompson,Wen Xiao Zhang,Ruixiu Wang,Rose M. Cubbon,Edward A. O'Neill,Jeffrey J. Hale
标识
DOI:10.1016/j.bmcl.2015.09.016
摘要
Several series of novel non-thiourea-containing aminopyrazine derivatives were designed based on the MK-2 inhibitors 1-(2-aminopyrazin-3-yl)methyl-2-thioureas. These compounds were synthesized and evaluated for their inhibitory activity against MK-2 enzyme in vitro. Compounds with low micromolar to sub-micromolar IC50 values were identified, and several compounds were also found to be active in suppressing the lipopolysaccharide (LPS)-stimulated TNFα production in THP-1 cells with minimum shift compared to their enzyme activity.
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