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Discovery of 4-((3′R,4′S,5′R)-6″-Chloro-4′-(3-chloro-2-fluorophenyl)-1′-ethyl-2″-oxodispiro[cyclohexane-1,2′-pyrrolidine-3′,3″-indoline]-5′-carboxamido)bicyclo[2.2.2]octane-1-carboxylic Acid (AA-115/APG-115): A Potent and Orally Active Murine Double Minute 2 (MDM2) Inhibitor in Clinical Development

[Image: see text] We previously reported the design of spirooxindoles with two identical substituents at the carbon-2 of the pyrrolidine core as potent MDM2 inhibitors. In this paper we describe an extensive structure–activity relationship study of this class of MDM2 inhibitors, which led to the dis...

وصف كامل

محفوظ في:
التفاصيل البيبلوغرافية
الحاوية / القاعدة:J Med Chem
المؤلفون الرئيسيون: Aguilar, Angelo, Lu, Jianfeng, Liu, Liu, Du, Ding, Bernard, Denzil, McEachern, Donna, Przybranowski, Sally, Li, Xiaoqin, Luo, Ruijuan, Wen, Bo, Sun, Duxin, Wang, Hengbang, Wen, Jianfeng, Wang, Guangfeng, Zhai, Yifan, Guo, Ming, Yang, Dajun, Wang, Shaomeng
التنسيق: Artigo
اللغة:Inglês
منشور في: American Chemical Society 2017
الوصول للمادة أونلاين:https://ncbi.nlm.nih.gov/pmc/articles/PMC5394527/
https://ncbi.nlm.nih.gov/pubmed/28339198
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b01665
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