2. Academic Validation
  3. BMS-871: a novel orally active pan-Notch inhibitor as an anticancer agent

BMS-871: a novel orally active pan-Notch inhibitor as an anticancer agent

  • Bioorg Med Chem Lett. 2015 May 1;25(9):1905-9. doi: 10.1016/j.bmcl.2015.03.038.
Weifang Shan 1,  Aaron Balog 2,  Claude Quesnelle 2,  Patrice Gill 2,  Wen-Ching Han 2,  Derek Norris 2,  Sunilkumar Mandal 3,  Raja Thiruvenkadam 3,  Kiran Babu Gona 3,  Kamalraj Thiyagarajan 3,  Sathiah Kandula 3,  Kelly McGlinchey 2,  Krista Menard 2,  Mei-Li Wen 2,  Anne Rose 2,  Ronald White 2,  Victor Guarino 2,  Ding Ren Shen 2,  Mary Ellen Cvijic 2,  Asoka Ranasinghe 2,  Jun Dai 2,  Yingru Zhang 2,  Dauh-Rurng Wu 2,  Arvind Mathur 2,  Richard Rampulla 2,  George Trainor 2,  John T Hunt 2,  Gregory D Vite 2,  Richard Westhouse 2,  Francis Y Lee 2,  Ashvinikumar V Gavai 2
Affiliations

Affiliations

  • 1 Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States. Electronic address: weifang.shan@bms.com.
  • 2 Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • 3 Biocon BMS Research and Development Center (BBRC), Syngene International Ltd, Plot No. 2 & 3, Bommasandra IV Phase, Jigani Link Road, Bangalore 560 099, India.
PMID: 25857941 DOI: 10.1016/j.bmcl.2015.03.038
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.

Keywords

Anticancer; Notch inhibitor; T-acute lymphoblastic leukemia; Triple-negative breast cancer.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-120372
    泛Notch抑制剂
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