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...

Descripción completa

Detalles Bibliográficos
Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2017
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5394527/
https://www.ncbi.nlm.nih.gov/pubmed/28339198
http://dx.doi.org/10.1021/acs.jmedchem.6b01665

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5394527/
https://www.ncbi.nlm.nih.gov/pubmed/28339198
http://dx.doi.org/10.1021/acs.jmedchem.6b01665

Ejemplares similares