N-叔丁氧羰基-3-(4-联苯基)-L-丙氨酸置于三乙胺,Sodium Tetrahydroborate体系中,用 四氢呋喃,水 用作溶剂,化学反应 0.25H,以77%的收率获得1426129-50-1对映异构体
参考文献:New Thiazole Carboxamides As Potent Inhibitors Of Akt Kinases
标题:New Thiazole Carboxamides As Potent Inhibitors Of Akt Kinases
摘要:A New Series Of 2-Substituted Thiazole Carboxamides Were Identified As Potent Pan Inhibitors Against All Three Isoforms Of Akt (Akt1,Akt2 And Akt3) By Systematic Optimization Of Weak Screening Hit N-(1-Amino-3-Phenylpropan-2-yl)-2-Phenylthiazole-5-Carboxamide (1). One Of The Most Potent Compounds,5M,Inhibited The Kinase Activities Of Akt1,Akt2 And Akt3 With Ic50 Values Of 25,196 And 24 Nm,Respectively. The Compound Also Potently Inhibited The Phosphorylation Of Downstream Mdm2 And Gsk3 Beta Proteins,And Displayed Strongly Antiproliferative Activity In Prostate Cancer Cells. The Inhibitors Might Serve As Lead Compounds For Further Development Of Novel Effective Anticancer Agents. (C) 2011 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2011.11.080