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.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4434460 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.5b00001 | DOI Listing |
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