1183321-00-7Relevant articles and documents
Discovery of potent and simplified piperidinone-based inhibitors of the MDM2-p53 interaction
Yu, Ming,Wang, Yingcai,Zhu, Jiang,Bartberger, Michael D.,Canon, Jude,Chen, Ada,Chow, David,Eksterowicz, John,Fox, Brian,Fu, Jiasheng,Gribble, Michael,Huang, Xin,Li, Zhihong,Liu, Jiwen,Lo, Mei-Chu,McMinn, Dustin,Oliner, Jonathan D.,Osgood, Tao,Rew, Yosup,Saiki, Anne Y.,Shaffer, Paul,Yan, Xuelei,Ye, Qiuping,Yu, Dongyin,Zhao, Xiaoning,Zhou, Jing,Olson, Steven H.,Medina, Julio C.,Sun, Daqing
supporting information, p. 894 - 899 (2014/09/17)
Continued optimization of the N-substituent in the piperidinone series provided potent piperidinone-pyridine inhibitors 6, 7, 14, and 15 with improved pharmacokinetic properties in rats. Reducing structure complexity of the N-alkyl substituent led to the discovery of 23, a potent and simplified inhibitor of MDM2. Compound 23 exhibits excellent pharmacokinetic properties and substantial in vivo antitumor activity in the SJSA-1 osteosarcoma xenograft mouse model.
