1352065-01-0Relevant academic research and scientific papers
Structure-based design of novel inhibitors of the MDM2-p53 interaction
Rew, Yosup,Sun, Daqing,Gonzalez-Lopez De Turiso, Felix,Bartberger, Michael D.,Beck, Hilary P.,Canon, Jude,Chen, Ada,Chow, David,Deignan, Jeffrey,Fox, Brian M.,Gustin, Darin,Huang, Xin,Jiang, Min,Jiao, Xianyun,Jin, Lixia,Kayser, Frank,Kopecky, David J.,Li, Yihong,Lo, Mei-Chu,Long, Alexander M.,Michelsen, Klaus,Oliner, Jonathan D.,Osgood, Tao,Ragains, Mark,Saiki, Anne Y.,Schneider, Steve,Toteva, Maria,Yakowec, Peter,Yan, Xuelei,Ye, Qiuping,Yu, Dongyin,Zhao, Xiaoning,Zhou, Jing,Medina, Julio C.,Olson, Steven H.
, p. 4936 - 4954 (2012/08/07)
Structure-based rational design led to the discovery of novel inhibitors of the MDM2-p53 protein-protein interaction. The affinity of these compounds for MDM2 was improved through conformational control of both the piperidinone ring and the appended N-alkyl substituent. Optimization afforded 29 (AM-8553), a potent and selective MDM2 inhibitor with excellent pharmacokinetic properties and in vivo efficacy.
PIPERIDINONE DERIVATIVES AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER
-
Page/Page column 466-467, (2011/12/14)
The present invention provides MDM2 inhibitor compounds of Formula (I), wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
