| Autor: |
Claude A. Quesnelle, Patrice Gill, Richard Rampulla, Ching Su, Gerry Everlof, George L. Trainor, Ke Chen, Vinod Arora, Richard A. Westhouse, Celia D’Arienzo, Andrew J. Tebben, Weifang Shan, John T. Hunt, Derek J. Norris, Louis J. Lombardo, Zheng Yang, Arvind Mathur, Mei-Li Wen, Yingru Zhang, Dauh-Rurng Wu, Wen-Ching Han, Krista Menard, Victor R. Guarino, Asoka Ranasinghe, Richard E. Olson, Ashvinikumar V. Gavai, Bruce S. Fischer, Phil S. Baran, Anne Rose, Lan Xiao, Ronald E. White, Mary Ellen Cvijic, Gregory D. Vite, Ding Ren Shen, Jere E. Meredith, Haiqing Wang, Francis Y. Lee, Aaron Balog |
| Rok vydání: |
2015 |
| Předmět: |
|
| Zdroj: |
ACS Medicinal Chemistry Letters. 6:523-527 |
| ISSN: |
1948-5875 |
| DOI: |
10.1021/acsmedchemlett.5b00001 |
| Popis: |
Structure-activity relationships in a series of (2-oxo-1,4-benzodiazepin-3-yl)-succinamides identified highly potent inhibitors of γ-secretase mediated signaling of Notch1/2/3/4 receptors. On the basis of its robust in vivo efficacy at tolerated doses in Notch driven leukemia and solid tumor xenograft models, 12 (BMS-906024) was selected as a candidate for clinical evaluation. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
|
