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  1. AU="Thiyagarajan, Kamalraj"
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  1. Article ; Online: Discovery of (

    Luo, Guanglin / Chen, Ling / Kostich, Walter A / Hamman, Brian / Allen, Jason / Easton, Amy / Bourin, Clotilde / Gulianello, Michael / Lippy, Jonathan / Nara, Susheel / Maishal, Tarun Kumar / Thiyagarajan, Kamalraj / Jalagam, Prasadrao / Pattipati, Sreenivasulu Naidu / Dandapani, Kumaran / Dokania, Manoj / Vattikundala, Pradeep / Sharma, Vivek / Elavazhagan, Saravanan /
    Verma, Manoj Kumar / Das, Manish Lal / Wagh, Santosh / Balakrishnan, Anand / Johnson, Benjamin M / Santone, Kenneth S / Thalody, George / Denton, Rex / Saminathan, Hariharan / Holenarsipur, Vinay K / Kumar, Anoop / Rao, Abhijith / Putlur, Siva Prasad / Sarvasiddhi, Sarat Kumar / Shankar, Ganesh / Louis, Justin V / Ramarao, Manjunath / Conway, Charles M / Li, Yu-Wen / Pieschl, Rick / Tian, Yuan / Hong, Yang / Ditta, Jonathan / Mathur, Arvind / Li, Jianqing / Smith, Daniel / Pawluczyk, Joseph / Sun, Dawn / Yip, Shiuhang / Wu, Dauh-Rurng / Vetrichelvan, Muthalagu / Gupta, Anuradha / Wilson, Alan / Gopinathan, Suma / Wason, Suman / Bristow, Linda / Albright, Charles F / Bronson, Joanne J / Macor, John E / Dzierba, Carolyn D

    Journal of medicinal chemistry

    2022  Volume 65, Issue 6, Page(s) 4457–4480

    Abstract: Recent mouse knockout studies identified adapter protein-2 associated kinase 1 (AAK1) as a viable target for treating neuropathic pain. Potent small-molecule inhibitors of AAK1 have been identified and show efficacy in various rodent pain models. ( ...

    Abstract Recent mouse knockout studies identified adapter protein-2 associated kinase 1 (AAK1) as a viable target for treating neuropathic pain. Potent small-molecule inhibitors of AAK1 have been identified and show efficacy in various rodent pain models. (
    MeSH term(s) Amines ; Animals ; Brain ; Mice ; Neuralgia/drug therapy ; Protein Kinase Inhibitors/pharmacology ; Protein Kinase Inhibitors/therapeutic use ; Rats ; Spinal Cord
    Chemical Substances Amines ; Protein Kinase Inhibitors
    Language English
    Publishing date 2022-03-08
    Publishing country United States
    Document type Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.1c02131
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: 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

    Bioorganic & medicinal chemistry letters

    2015  Volume 25, Issue 9, Page(s) 1905–1909

    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) ...

    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.
    MeSH term(s) Administration, Oral ; Animals ; Antineoplastic Agents/administration & dosage ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Benzodiazepinones/administration & dosage ; Benzodiazepinones/chemistry ; Benzodiazepinones/pharmacology ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Humans ; Mice ; Microsomes, Liver/drug effects ; Microsomes, Liver/metabolism ; Molecular Structure ; Neoplasms, Experimental/drug therapy ; Neoplasms, Experimental/metabolism ; Neoplasms, Experimental/pathology ; Receptors, Notch/antagonists & inhibitors ; Receptors, Notch/metabolism ; Structure-Activity Relationship
    Chemical Substances Antineoplastic Agents ; BMS-871 ; Benzodiazepinones ; Receptors, Notch
    Language English
    Publishing date 2015-05-01
    Publishing country England
    Document type Journal Article
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2015.03.038
    Database MEDical Literature Analysis and Retrieval System OnLINE

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