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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Detalles Bibliográficos
Autores principales: 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: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2020
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7549103/
https://www.ncbi.nlm.nih.gov/pubmed/33062160
http://dx.doi.org/10.1021/acsmedchemlett.9b00568

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