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📜2-苯基吡啶-4-羧酸甲酯置于lithium Hydroxide体系中,用 四氢呋喃,甲醇 作为反应溶剂,化学反应 2.0H,反应生成 2-苯基-吡啶-4-甲酸
参考文献:Start Selective And Rigidify: The Discovery Path Toward A Next Generation Of Egfr Tyrosine Kinase Inhibitors
标题:Start Selective And Rigidify: The Discovery Path Toward A Next Generation Of Egfr Tyrosine Kinase Inhibitors
摘要:The Epidermal Growth Factor Receptor (Egfr),When Carrying An Activating Mutation Like Del19 Or L858R,Acts As An Oncogenic Driver In A Subset Of Lung Tumors. While Tumor Responses To Tyrosine Kinase Inhibitors (Tkis) Are Accompanied By Marked Tumor Shrinkage,The Response Is Usually Not Durable. Most Patients Relapse Within Two Years Of Therapy Often Due To Acquisition Of An Additional Mutation In Egfr Kinase Domain That Confers Resistance To Tkis. Crucially,Oncogenic Egfr Harboring Both Resistance Mutations,T790M And C797S,Can No Longer Be Inhibited By Currently Approved Egfr Tkis. Here,We Describe The Discovery Of Bi-4020,Which Is A Noncovalent,Wild-Type Egfr Sparing,Macro-Cyclic Tki. Bi-4020 Potently Inhibits The Above-Described Egfr Variants And Induces Tumor Regressions In A Cross-Resistant Egfr(Del19 T790M C797S) Xenograft Model. Key Was The Identification Of A Highly Selective But Moderately Potent Benzimidazole Followed By Complete Rigidification Of The Molecule Through Macrocyclization.
DOI:10.1021/acs.Jmedchem.9B01169