2,5-二溴苯甲酸置于氯化亚砜,硼烷四氢呋喃络合物,硫酸,Lithium Chloride体系中,用 四氢呋喃,二甲基亚砜,N,N-二甲基甲酰胺 用作溶剂,化学反应 52.4H,反应生成2,5-二溴苯乙酸
参考文献:Aminopyridine-Based C-Jun N-Terminal Kinase Inhibitors With Cellular Activity And Minimal Cross-Kinase Activity
标题:Aminopyridine-Based C-Jun N-Terminal Kinase Inhibitors With Cellular Activity And Minimal Cross-Kinase Activity
摘要:The C-Jun N-Terminal Kinases (Jnk-1,-2,And-3) Are Members Of The Mitogen Activated Protein (Map) Kinase Family Of Enzymes. They Are Activated In Response To Certain Cytokines,As Well As By Cellular Stresses Including Chemotoxins,Peroxides,And Irradiation. They Have Been Implicated In The Pathology Of A Variety Of Different Diseases With An Inflammatory Component Including Asthma,Stroke,Alzheimer'S Disease,And Type 2 Diabetes Mellitus. In This Work,High-Throughput Screening Identified A Jnk Inhibitor With An Excellent Kinase Selectivity Profile. Using X-Ray Crystallography And Biochemical Screening To Guide Our Lead Optimization,We Prepared Compounds With Inhibitory Potencies In The Low-Double-Digit Nanomolar Range,Activity In Whole Cells,And Pharmacokinetics Suitable For In Vivo Use. The New Compounds Were Over 1,000-Fold Selective For Jnk-1 And-2 Over Other Map Kinases Including Erk2,P38Alpha,And P38Delta And Showed Little Inhibitory Activity Against A Panel Of 74 Kinases.
Doi:10.1021/jm060199B