Goldberg D R, Choi Y, Cogan D, Corson M, DeLeon R, Gao A, Gruenbaum L, Hao M H, Joseph D, Kashem M A, Miller C, Moss N, Netherton M R, Pargellis C P, Pelletier J, Sellati R, Skow D, Torcellini C, Tseng Y-C, Wang J, Wasti R, Werneburg B, Wu J P, Xiong Z
Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc., Research and Development Center, 900 Ridgebury Road, Ridgefield, CT 06877, USA.
Bioorg Med Chem Lett. 2008 Feb 1;18(3):938-41. doi: 10.1016/j.bmcl.2007.12.037. Epub 2007 Dec 23.
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.
丝裂原活化蛋白激酶激活的蛋白激酶 2（MK2）的吡嗪并吲哚酮抑制剂的优化实现了细胞活性与理化性质之间的合理平衡。机制研究支持对 MK2 的抑制作用，这是亚微摩尔级细胞功效的原因所在。
