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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Publicat a:ACS Med Chem Lett
Autors principals: 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
Format: Artigo
Idioma:Inglês
Publicat: American Chemical Society 2020
Accés en línia: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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