280581-64-8Relevant academic research and scientific papers
Discovery of a B-Cell Lymphoma 6 Protein-Protein Interaction Inhibitor by a Biophysics-Driven Fragment-Based Approach
Kamada, Yusuke,Sakai, Nozomu,Sogabe, Satoshi,Ida, Koh,Oki, Hideyuki,Sakamoto, Kotaro,Lane, Weston,Snell, Gyorgy,Iida, Motoo,Imaeda, Yasuhiro,Sakamoto, Junichi,Matsui, Junji
, p. 4358 - 4368 (2017/06/05)
B-cell lymphoma 6 (BCL6) is a transcriptional factor that expresses in lymphocytes and regulates the differentiation and proliferation of lymphocytes. Therefore, BCL6 is a therapeutic target for autoimmune diseases and cancer treatment. This report presen
AURORA KINASE AND JANUS KINASE INHIBITORS FOR PREVENTION OF GRAFT VERSUS HOST DISEASE
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Page/Page column 51, (2017/09/28)
Disclosed herein are compounds and methods for reducing the risk of developing, preventing, or treating graft versus host disease (GVHD) in a subject. The compounds can concurrently block Aurora kinase A and JAK2 signal transduction which synergistically suppresses alloreactive human T-cells in vitro, prevents xenogeneic graft- versus-host disease without impairing anti-tumor responses, and promotes the development and suppressive potency of CD39+ inducible Treg. In certain aspects, disclosed are compounds of Formula I-V.
Design, Synthesis, and Antitumor Evaluation of 4-Amino-(1H)-pyrazole Derivatives as JAKs Inhibitors
Liang, Xuewu,Zang, Jie,Zhu, Mengyuan,Gao, Qianwen,Wang, Binghe,Xu, Wenfang,Zhang, Yingjie
supporting information, p. 950 - 955 (2016/10/22)
Abnormalities in the JAK/STAT signaling pathway lead to many diseases such as immunodeficiency, inflammation, and cancer. Herein, we designed and synthesized a series of 4-amino-(1H)-pyrazole derivatives as potent JAKs inhibitors for cancer treatment. Res
Facile and regioselective synthesis of novel 2,4-disubstituted-5- fluoropyrimidines as potential kinase inhibitors
Wada, Hiroki,Cheng, Lili,Jiang, Ji,Jiang, Zhigan,Xie, Jun,Hu, Tao,Sanganee, Hitesh,Luker, Tim
scheme or table, p. 1720 - 1724 (2012/05/04)
2,4-Disubstituted-5-fluoropyrimidine is a biologically active molecular core seen in various anticancer agents such as 5-fluorouracil (5-FU). As part of a programme aimed at discovering kinase inhibitors, routes to two series of novel compounds (5-fluorop
Process for the identification of novel enzyme interacting compounds
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, (2009/10/01)
The present invention relates to methods for the characterization of enzymes or of enzyme-compound complexes, wherein the enzyme is obtained from a protein preparation with the help of at least one broad spectrum ligand immobilized on a solid support and wherein the enzyme is characterized by mass spectrometry. These methods are useful for the screening of non-immobilized compound libraries, selectivity profiling of lead compounds and mechanism of action studies in living cells.
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: Identification and optimisation of substituted 2,4-bis anilino pyrimidines
Breault, Gloria A.,Ellston, Rebecca P. A.,Green, Stephen,James, S. Russell,Jewsbury, Philip J.,Midgley, Catherine J.,Pauptit, Richard A.,Minshull, Claire A.,Tucker, Julie A.,Pease, J. Elizabeth
, p. 2961 - 2966 (2007/10/03)
Through chemical modification and X-ray crystallography we identified the 2,4-bis anilino pyrimidines as potent inhibitors of CDK4. Herein, we describe the optimisation of this series.
