Liu Mei, Wang Sanyi, Clampit Jill E, Gum Rebecca J, Haasch Deanna L, Rondinone Cristina M, Trevillyan James M, Abad-Zapatero Cele, Fry Elizabeth H, Sham Hing L, Liu Gang
Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064-6098, USA.
Bioorg Med Chem Lett. 2007 Feb 1;17(3):668-72. doi: 10.1016/j.bmcl.2006.10.093. Epub 2006 Nov 2.
A new series of 4-anilinopyrimidines has been synthesized and evaluated as JNK1 inhibitors. SAR studies led to the discovery of potent JNK1 inhibitors with good enzymatic activity as well as cellular potency represented by compound 2b. Kinase selectivity profile and the crystal structure of 2b are also described.
已经合成了一系列新的4-苯胺基嘧啶并将其作为JNK1抑制剂进行评估。构效关系（SAR）研究发现了具有良好酶活性以及细胞活性的强效JNK1抑制剂，化合物2b就是代表。文中还描述了2b的激酶选择性概况和晶体结构。
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