Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1370876 | Bioorganic & Medicinal Chemistry Letters | 2015 | 5 Pages |
Abstract
This Letter describes synthesis, SAR, and biological activity of (2-oxo-1,4-benzodiazepin-3-yl)-succinamides as inhibitors of γ-secretase mediated signaling of Notch receptors. Optimization of this series led to the identification of BMS-871 (compound 30) which displayed robust in vivo efficacy in Notch-dependent leukemia and solid tumor xenograft models.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Weifang Shan, Aaron Balog, Claude Quesnelle, Patrice Gill, Wen-Ching Han, Derek Norris, Sunilkumar Mandal, Raja Thiruvenkadam, Kiran Babu Gona, Kamalraj Thiyagarajan, Sathiah Kandula, Kelly McGlinchey, Krista Menard, Mei-Li Wen, Anne Rose, Ronald White,