التفاصيل البيبلوغرافية
العنوان:
BMS-871: A novel orally active pan-Notch inhibitor as an anticancer agent
المؤلفون:
George L. Trainor , Jun Dai , Arvind Mathur , Francis Y. Lee , Sunilkumar Mandal , Yingru Zhang , Richard Rampulla , Kiran Babu Gona , Patrice Gill , Raja Thiruvenkadam , Victor R. Guarino , Wen-Ching Han , Ding Ren Shen , Aaron Balog , Mary Ellen Cvijic , Dauh-Rurng Wu , Gregory D. Vite , Krista Menard , Anne Rose , Sathiah Kandula , Ashvinikumar V. Gavai , Weifang Shan , John T. Hunt , Asoka Ranasinghe , Kelly McGlinchey , Richard A. Westhouse , Claude A. Quesnelle , Derek J. Norris , Mei-Li Wen , Ronald E. White , Kamalraj Thiyagarajan
المصدر:
Bioorganic & Medicinal Chemistry Letters . 25:1905-1909
بيانات النشر:
Elsevier BV, 2015.
سنة النشر:
2015
مصطلحات موضوعية:
Clinical Biochemistry , Administration, Oral , Pharmaceutical Science , Antineoplastic Agents , Pharmacology , Biochemistry , Mice , Structure-Activity Relationship , In vivo , Cell Line, Tumor , Drug Discovery , medicine , Animals , Humans , Receptor , Solid tumor , Molecular Biology , Cell Proliferation , Benzodiazepinones , Dose-Response Relationship, Drug , Molecular Structure , Receptors, Notch , Chemistry , Organic Chemistry , Biological activity , Neoplasms, Experimental , medicine.disease , Leukemia , Orally active , Microsomes, Liver , Molecular Medicine , Drug Screening Assays, Antitumor
الوصف:
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.
تدمد:
0960-894X
URL الوصول:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8122d9a6071f4288b3ad5fa62172ff7c https://doi.org/10.1016/j.bmcl.2015.03.038
حقوق:
CLOSED
رقم الأكسشن:
edsair.doi.dedup.....8122d9a6071f4288b3ad5fa62172ff7c
قاعدة البيانات:
OpenAIRE
