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BMS-871: a novel orally active pan-Notch inhibitor as an anticancer agent.
Shan, Weifang; Balog, Aaron; Quesnelle, Claude; Gill, Patrice; Han, Wen-Ching; Norris, Derek; Mandal, Sunilkumar; Thiruvenkadam, Raja; Gona, Kiran Babu; Thiyagarajan, Kamalraj; Kandula, Sathiah; McGlinchey, Kelly; Menard, Krista; Wen, Mei-Li; Rose, Anne; White, Ronald; Guarino, Victor; Shen, Ding Ren; Cvijic, Mary Ellen; Ranasinghe, Asoka; Dai, Jun; Zhang, Yingru; Wu, Dauh-Rurng; Mathur, Arvind; Rampulla, Richard; Trainor, George; Hunt, John T; Vite, Gregory D; Westhouse, Richard; Lee, Francis Y; Gavai, Ashvinikumar V.
Afiliación
  • Shan W; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States. Electronic address: weifang.shan@bms.com.
  • Balog A; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Quesnelle C; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Gill P; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Han WC; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Norris D; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Mandal S; Biocon BMS Research and Development Center (BBRC), Syngene International Ltd, Plot No. 2 & 3, Bommasandra IV Phase, Jigani Link Road, Bangalore 560 099, India.
  • Thiruvenkadam R; Biocon BMS Research and Development Center (BBRC), Syngene International Ltd, Plot No. 2 & 3, Bommasandra IV Phase, Jigani Link Road, Bangalore 560 099, India.
  • Gona KB; Biocon BMS Research and Development Center (BBRC), Syngene International Ltd, Plot No. 2 & 3, Bommasandra IV Phase, Jigani Link Road, Bangalore 560 099, India.
  • Thiyagarajan K; Biocon BMS Research and Development Center (BBRC), Syngene International Ltd, Plot No. 2 & 3, Bommasandra IV Phase, Jigani Link Road, Bangalore 560 099, India.
  • Kandula S; Biocon BMS Research and Development Center (BBRC), Syngene International Ltd, Plot No. 2 & 3, Bommasandra IV Phase, Jigani Link Road, Bangalore 560 099, India.
  • McGlinchey K; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Menard K; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Wen ML; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Rose A; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • White R; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Guarino V; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Shen DR; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Cvijic ME; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Ranasinghe A; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Dai J; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Zhang Y; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Wu DR; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Mathur A; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Rampulla R; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Trainor G; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Hunt JT; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Vite GD; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Westhouse R; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Lee FY; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
  • Gavai AV; Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543, United States.
Bioorg Med Chem Lett ; 25(9): 1905-9, 2015 May 01.
Article en En | MEDLINE | ID: mdl-25857941
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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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Benzodiazepinonas / Receptores Notch / Antineoplásicos Límite: Animals / Humans Idioma: En Año: 2015 Tipo del documento: Article
Texto completo
Imprimir
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PubMed Links
Buscar en Google

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Benzodiazepinonas / Receptores Notch / Antineoplásicos Límite: Animals / Humans Idioma: En Año: 2015 Tipo del documento: Article