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Imidazo[1,2-b]pyridazines as inhibitors of DYRK kinases
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2024-03-07 , DOI: 10.1016/j.ejmech.2024.116292 Scott H Henderson 1 , Fiona J Sorrell 2 , James M Bennett 3 , Oleg Fedorov 2 , Marcus T Hanley 4 , Paulo H Godoi 5 , Roberta Ruela de Sousa 5 , Sean Robinson 6 , Iva Hopkins Navratilova 7 , Jonathan M Elkins 8 , Simon E Ward 4
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2024-03-07 , DOI: 10.1016/j.ejmech.2024.116292 Scott H Henderson 1 , Fiona J Sorrell 2 , James M Bennett 3 , Oleg Fedorov 2 , Marcus T Hanley 4 , Paulo H Godoi 5 , Roberta Ruela de Sousa 5 , Sean Robinson 6 , Iva Hopkins Navratilova 7 , Jonathan M Elkins 8 , Simon E Ward 4
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Selective inhibitors of DYRK1A are of interest for the treatment of cancer, Type 2 diabetes and neurological disorders. Optimization of imidazo [1,2-]pyridazine through structure−activity relationship exploration and drug design efforts led to the discovery of as a potent cellular inhibitor of DYRK1A with selectivity over much of the kinome. The binding mode of was elucidated with X-ray crystallography, facilitating the rational design of , an imidazo [1,2-]pyridazine with improved kinase selectivity with respect to closely related CLK kinases.
中文翻译:
咪唑并[1,2-b]哒嗪作为 DYRK 激酶抑制剂
DYRK1A 的选择性抑制剂可用于治疗癌症、2 型糖尿病和神经系统疾病。通过构效关系探索和药物设计工作对咪唑并[1,2-]哒嗪进行优化,结果发现它是一种有效的 DYRK1A 细胞抑制剂,对大部分激酶组具有选择性。通过 X 射线晶体学阐明了 的结合模式,有助于合理设计 ,一种咪唑并[1,2-]哒嗪,其对密切相关的 CLK 激酶具有改进的激酶选择性。
更新日期:2024-03-07
中文翻译:
![](https://scdn.x-mol.com/jcss/images/paperTranslation.png)
咪唑并[1,2-b]哒嗪作为 DYRK 激酶抑制剂
DYRK1A 的选择性抑制剂可用于治疗癌症、2 型糖尿病和神经系统疾病。通过构效关系探索和药物设计工作对咪唑并[1,2-]哒嗪进行优化,结果发现它是一种有效的 DYRK1A 细胞抑制剂,对大部分激酶组具有选择性。通过 X 射线晶体学阐明了 的结合模式,有助于合理设计 ,一种咪唑并[1,2-]哒嗪,其对密切相关的 CLK 激酶具有改进的激酶选择性。