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...

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Veröffentlicht in:J Med Chem
Hauptverfasser: 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
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Chemical Society 2017
Online Zugang: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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