CAS: 1158838-45-9; N-(2-Chlorophenyl)-4-((2-((4-(2-(4-Ethylpiperazin-1-yl)-2-Oxoethyl)Phenyl)Amino)-5-Fluoropyrimidin-4-yl)Amino)Benzamide

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CAS号5308-25-8 N-乙基哌嗪 | CAS号1158838-42-6 4-[[4-[[4-[[(2-...

📜N-乙基哌嗪,4-[[4-[[4-[[(2-氯苯基)氨基]羰基]苯基] 氨基]-5-氟-2-嘧啶]氨基]苯乙酸置于o-(Benzotriazol-1-yl)-N,N,N',N'-Tetramethyluronium Tetrafluoroborate,N,N-二异丙基乙胺体系中,用 N,N-二甲基甲酰胺 用作溶剂,以78%的收率获得n-(2-氯苯基)-4-(2-(4-(2-(4-乙基哌嗪-1-基)-2-氧代乙基)苯基氨基)-5-氟嘧啶-4-基氨基)苯甲酰胺
参考文献:A Class Of 2,4-Bisanilinopyrimidine Aurora A Inhibitors With Unusually High Selectivity Against Aurora B
标题:A Class Of 2,4-Bisanilinopyrimidine Aurora A Inhibitors With Unusually High Selectivity Against Aurora B
摘要:The Two Major Aurora Kinases Carry Out Critical Functions At Distinct Mitotic Stages. Selective Inhibitors Of These Kinases,As Well As Pan-Aurora Inhibitors,Show Antitumor Efficacy And Are Now Under Clinical Investigation. However,The Atp-Binding Sites Of Aurora A And Aurora B Are Virtually Identical,And The Structural Basis For Selective Inhibition Has Therefore Not Been Clear. We Report Here A Class Of Bisanilinopyrimidine Aurora A Inhibitors With Excellent Selectivity For Aurora A Over Aurora B,Both In Enzymatic Assays And In Cellular Phenotypic Assays. Crystal Structures Of Two Of The Inhibitors In Complex With Aurora A Implicate A Single Amino Acid Difference In Aurora B As Responsible For Poor Inhibitory Activity Against This Enzyme. Mutation Of This Residue In Aurora B (E161T) Or Aurora A (T217E) Is Sufficient To Swap The Inhibition Profile,Suggesting That This Difference Might Be Exploited More Generally To Achieve High Selectivity For Aurora A.
Doi:10.1021/jm9000314