Article ID Journal Published Year Pages File Type
1370876 Bioorganic & Medicinal Chemistry Letters 2015 5 Pages PDF
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.

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Physical Sciences and Engineering Chemistry Organic Chemistry
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