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Pyrazinoindolone inhibitors of MAPKAP-K2

D.R. Goldberg,Y. Choi,D. Cogan,M. Corson,R. DeLeon,A. Gao,L. Gruenbaum,M.H. Hao,D. Joseph,M.A. Kashem,C. Miller,N. Moss,M.R. Netherton,C.P. Pargellis,J. Pelletier,R. Sellati,D. Skow,C. Torcellini,Y.-C. Tseng, J. Wang,R. Wasti,B. Werneburg,J.P. Wu,Z. Xiong

Bioorganic & Medicinal Chemistry Letters（2008）

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摘要
Optimization of pyrazinoindolone inhibitors of MAPKAP-K2 (MK2) provides a reasonable balance of cellular potency and physicochemical properties. Mechanistic studies support the inhibition of MK2 which is responsible for the sub-micromolar cellular efficacy.
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关键词
MAPKAP-K2,THP-1
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