Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X(L) Inhibitor

[Image: see text] Herein we describe the discovery of A-1331852, a first-in-class orally active BCL-X(L) inhibitor that selectively and potently induces apoptosis in BCL-X(L)-dependent tumor cells. This molecule was generated by re-engineering our previously reported BCL-X(L) inhibitor A-1155463 usi...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Wang, Le, Doherty, George A., Judd, Andrew S., Tao, Zhi-Fu, Hansen, T. Matthew, Frey, Robin R., Song, Xiaohong, Bruncko, Milan, Kunzer, Aaron R., Wang, Xilu, Wendt, Michael D., Flygare, John A., Catron, Nathaniel D., Judge, Russell A., Park, Chang H., Shekhar, Shashank, Phillips, Darren C., Nimmer, Paul, Smith, Morey L., Tahir, Stephen K., Xiao, Yu, Xue, John, Zhang, Haichao, Le, Phuong N., Mitten, Michael J., Boghaert, Erwin R., Gao, Wenqing, Kovar, Peter, Choo, Edna F., Diaz, Dolores, Fairbrother, Wayne J., Elmore, Steven W., Sampath, Deepak, Leverson, Joel D., Souers, Andrew James
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2020
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC7549103/
https://ncbi.nlm.nih.gov/pubmed/33062160
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.9b00568
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