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CAS号1072-97-5 2-氨基-5-溴吡啶 | CAS号1004550-24-6 ethyl 2-chloro-... | CAS号474706-74-6 6-溴-3-碘咪唑并[1,2-A]吡啶 | CAS号541-41-3 氯甲酸乙酯 | CAS号33142-21-1 2-氯-3-氧代丙酸乙酯 | CAS号105-39-5 氯乙酸乙酯 | CAS号109-94-4 甲酸乙酯 | CAS号944896-42-8 6-溴咪唑并[1,2-a]吡啶-3-羧酸

📜2-氨基-5-溴吡啶置于碳酸氢钠体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 6.0H,反应生成 6-溴咪唑并[1,2-A]吡啶-3-羧酸乙酯
参考文献:发现 3,6-二取代的咪唑并[1,2-A]吡啶衍生物作为一类新的 Clk1 抑制剂
标题:发现 3,6-二取代的咪唑并[1,2-A]吡啶衍生物作为一类新的 Clk1 抑制剂
摘要:抑制 Cdc2 样激酶 1 (Clk1) 可以有效地诱导自噬,它被认为是治疗自噬相关疾病的潜在靶点.在此我们报告发现了一系列 3,6-二取代的咪唑并[1,2-A]吡啶衍生物作为一类新的 Clk1 抑制剂.其中,化合物9E是最有效的一种,其对 Clk1 激酶的 Ic 50值为 4 Nm.在体外,该化合物降低了 Clk1 典型下游底物的磷酸化水平并影响它们的亚细胞重新分布.进一步研究表明,9E可有效诱导自噬.总的来说,这项研究为靶向 Clk1 激酶的药物发现提供了一种有前景的先导化合物.
DOI:10.1016/j.Bmcl.2021.127881

专利信息

专利号:WO-2011050245-A1
优先权日:2009-10-23
标 题:Bicyclic heteroaryls as kinase inhibitors
发明人：FENG YANGBO; CHEN YEN TING; SESSIONS HAMPTON; MISHRA JITENDRA K; CHOWDHURY SARWAT; YIN YAN; LOGRASSO PHILIP; LUO JUN-LI; BANNISTER THOMAS; SCHROETER THOMAS
权利人:FENG YANGBO; CHEN YEN TING; SESSIONS HAMPTON; MISHRA JITENDRA K; CHOWDHURY SARWAT; YIN YAN; LOGRASSO PHILIP; LUO JUN-LI; BANNISTER THOMAS; SCHROETER THOMAS
摘要:The invention is directed to heteroaryl compounds useful as inhibitors of various kinase enzymes. In various embodiments, the invention provides a heteroaryl compound having inhibitory bioactivity with respect to a Rho kinase, an AKT kinase, a p70S6K kinase, a LIM kinase, an IKK kinase, a Flt kinase, an Aurora kinase, or a Src kinase, or any combination thereof. Compounds of the invention include bicyclic heteroaryl compounds of formula (I), which can contain a bridging nitrogen atom at a ring junction. The invention further provides methods of synthesis of compounds of the invention, pharmaceutical compositions, pharmaceutical combinations, and methods of treatment of malconditions using compounds of the invention.