1304273-34-4Relevant academic research and scientific papers
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.
N-alkylation of lactams with secondary heterobenzylic bromides
Yu, Ming,Stevenson, Karis,Zhou, Gene
supporting information, p. 5591 - 5594 (2014/12/11)
We herein report a general N-alkylation reaction of lactams with secondary heterobenzylic bromides. This methodology features mild reaction condition, moderate to high product isolation yield, and broad substrate scope. Good chemical and structural tolerance has also been demonstrated by both the secondary heterobenzylic bromides and lactam substrates.
