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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Argitaratua izan da:ACS Med Chem Lett
Egile Nagusiak: 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.
Formatua: Artigo
Hizkuntza:Inglês
Argitaratua: American Chemical Society 2016
Sarrera elektronikoa: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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