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N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR |
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| Authors: | Deak Holly L Newcomb John R Nunes Joseph J Boucher Christina Cheng Alan C DiMauro Erin F Epstein Linda F Gallant Paul Hodous Brian L Huang Xin Lee Josie H Patel Vinod F Schneider Stephen Turci Susan M Zhu Xiaotian |
| Affiliation: | Department of Medicinal Chemistry, Amgen Inc., One Kendall Square, Building 1000, Cambridge, MA 02139, USA. holly.deak@amgen.com |
| Abstract: | N-3-(Phenylcarbamoyl)arylpyrimidine-5-carboxamides are a novel class of selective Lck inhibitors. This series of compounds derives its selectivity from a hydrogen bond with the gatekeeper Thr316 of the enzyme. X-ray co-crystal structural data, structure-activity relationships, and the synthesis of these inhibitors are reported herein. |
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