新型p53-hDM2抑制剂亮氨酸26位点上4-取代哌啶的构效关系研究
Structure-activity relationship study of 4-substituted piperidines at Leu26 moiety of novel p53-hDM2 inhibitors.
作者信息
Tian Yuan, Ma Yao, Gibeau Craig R, Lahue Brian R, Shipps Gerald W, Strickland Corey, Bogen Stéphane L
机构信息
Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
出版信息
Bioorg Med Chem Lett. 2016 Jun 1;26(11):2735-8. doi: 10.1016/j.bmcl.2016.03.078. Epub 2016 Mar 23.
Led by the structural information of the screening hit with mDM2 protein, a structure modification of Leu26 moiety of the novel p53-hDM2 inhibitors was conducted. A structure-activity relationship study of 4-substituted piperidines revealed compound 20t with good potencies and excellent CYP450 profiles.
以筛选得到的与mDM2蛋白结合的命中化合物的结构信息为指导，对新型p53-hDM2抑制剂的Leu26部分进行了结构修饰。对4-取代哌啶的构效关系研究表明，化合物20t具有良好的活性和出色的CYP450特性。
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