📜对溴甲苯置于potassium Permanganate,四(三苯基膦)钯,四丁基溴化铵,碘,Caesium Carbonate,Magnesium,Sodium Hydroxide体系中,用 四氢呋喃,水,乙腈 作为反应溶剂,化学反应 54.0H,反应生成 4-吡啶-3-基-苯甲酸 参考文献:Synthesis And Biological Evaluation Of Novel Aromatic-Heterocyclic Biphenyls As Potent Anti-Leukemia Agents 标题:Synthesis And Biological Evaluation Of Novel Aromatic-Heterocyclic Biphenyls As Potent Anti-Leukemia Agents 摘要:As A Continuation To Our Previous Research,Twenty-Eight Aromatic-Heterocyclic Biphenyls Were Designed And Synthesized As Novel Bcr-Abl Inhibitors. The Title Compounds Were Investigated For Their Anti-Proliferative Activities Against Wild K562 Cells And Imatinib-Resistant K562 Cells (K562R). The Results Indicated That Most Of Them Exhibited Potent Bcr-Abl Inhibition And Moderate Antiproliferative Potency Against K562 Cells. Furthermore,Three Compounds 3,7 And 21 Displayed Moderate Antiproliferative Activities Against K562R Cells. Molecular Docking Indicated That 3 Bound More Tightly With Bcr-Abl(T315I) Compared To Bcr-Abl(Wt). The Higher Affinity Was Consistent With Its Relatively Promising K562R Cell Growth Inhibition. These Aromatic-Heterocyclic Biphenyls Could Be Considered As Novel Lead Compound For Optimized As Bcr-Abl(T315I) Inhibitors. They Provide A Good Starting Point For The Further Development Of Novel Anti-Leukemia Agents Capable Of Dealing With Clinical Acquired Resistance Against Imatinib. (C) 2015 Elsevier Masson Sas. All Rights Reserved. DOI:10.1016/j.Ejmech.2015.07.015
参考标题:Design, Synthesis And Stepwise Optimization Of Nitrile-Based Inhibitors Of Cathepsins B And L 作者:Lorenzo Cianni,Fernanda Dos Reis Rocho,Vinícius Bonatto,Felipe Cardoso Prado Martins,Jerônimo Lameira,Andrei Leitão,Carlos A. Montanari,Anwar Shamim |发布日期:2021.1 摘要:Human Cathepsin B (Catb) Is An Important Biological Target In Cancer Therapy. In This Work, We Performed A Knowledge-Based Design Approach And The Synthesis Of A New Set Of 19 Peptide-Like Nitrile-Based Cathepsin Inhibitors. Reported Compounds Were Assayed Against A Panel Of Human Cysteine Proteases: Catb, Catl, Catk, And Cats. Three Compounds (7H, 7I, And 7J) Displayed Nanomolar Inhibition Of Catb
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参考文献:10.1021/acs.jmedchem.9b01582 摘要:Kwiatkowski J, Liu B, Pang S, Ahmad NHB, Wang G, Poulsen A, Yang H, Poh YR, Tee DHY, Ong E, Retna P, Dinie N, Kwek P, Wee JLK, Manoharan V, Low CB, Seah PG, Pendharkar V, Sangthongpitag K, Joy J, Baburajendran N, Jansson AE, Nacro K, Hill J, Keller TH, Hung AW. Stepwise Evolution of Fragment Hits against MAPK Interacting Kinases 1 and 2. J Med Chem. 2020 Jan 23;63(2):621–37. doi: 10.1021/acs.jmedchem.9b01582. 参考文献:10.1177/2472555219873068 摘要:Lee OW, Austin S, Gamma M, Cheff DM, Lee TD, Wilson KM, Johnson J, Travers J, Braisted JC, Guha R, Klumpp-Thomas C, Shen M, Hall MD. Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. SLAS Discov. 2020 Jan;25(1):9–20.