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Discovery of Potent and Simplified Piperidinone-Based Inhibitors of the MDM2–p53 Interaction

التفاصيل البيبلوغرافية
العنوان: Discovery of Potent and Simplified Piperidinone-Based Inhibitors of the MDM2–p53 Interaction
المؤلفون: Jiang Zhu, Tao Osgood, Xin Huang, Anne Y. Saiki, John Eksterowicz, Jiwen Jim Liu, Yosup Rew, Xiaoning Zhao, Qiuping Ye, Steven H. Olson, Julio C. Medina, Michael W. Gribble, David Chow, Jiasheng Fu, Ming Yu, Zhihong Li, Daqing Sun, Jude Canon, Dustin McMinn, Paul L. Shaffer, Xuelei Yan, Yingcai Wang, Brian M. Fox, Mei-Chu Lo, Jonathan D. Oliner, Dongyin Yu, Ada Chen, Michael D. Bartberger, Jing Zhou
المصدر: ACS Medicinal Chemistry Letters. 5:894-899
بيانات النشر: American Chemical Society (ACS), 2014.
سنة النشر: 2014
مصطلحات موضوعية: Antitumor activity, chemistry.chemical_compound, Pharmacokinetics, Chemistry, Stereochemistry, In vivo, Organic Chemistry, Drug Discovery, Substituent, Mdm2 p53, Biochemistry, Combinatorial chemistry
الوصف: 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.
تدمد: 1948-5875
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4ea38cb183b5572b76e6798f6302259b
https://doi.org/10.1021/ml500142b
حقوق: OPEN
رقم الأكسشن: edsair.doi.dedup.....4ea38cb183b5572b76e6798f6302259b
قاعدة البيانات: OpenAIRE
الوصف
تدمد:19485875