Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors

[Image: see text] A new subseries of substituted piperidines as p53-HDM2 inhibitors exemplified by 21 has been developed from the initial lead 1. Research focused on optimization of a crucial HDM2 Trp23–ligand interaction led to the identification of 2-(trifluoromethyl)thiophene as the preferred moi...

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Publicado en:ACS Med Chem Lett
Main Authors: Bogen, Stéphane L., Pan, Weidong, Gibeau, Craig R., Lahue, Brian R., Ma, Yao, Nair, Latha G., Seigel, Elise, Shipps, Gerald W., Tian, Yuan, Wang, Yaolin, Lin, Yinghui, Liu, Ming, Liu, Suxing, Mirza, Asra, Wang, Xiaoying, Lipari, Philip, Seidel-Dugan, Cynthia, Hicklin, Daniel J., Bishop, W. Robert, Rindgen, Diane, Nomeir, Amin, Prosise, Winifred, Reichert, Paul, Scapin, Giovanna, Strickland, Corey, Doll, Ronald J.
Formato: Artigo
Idioma:Inglês
Publicado: American Chemical Society 2016
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC4789661/
https://ncbi.nlm.nih.gov/pubmed/26985323
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00472
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