Discovery of 3-(4-sulfamoylnaphthyl)pyrazolo[1,5-a]pyrimidines as potent and selective ALK2 inhibitors

The pyrazolo[1,5-a]pyrimidine LDN-193189 is a potent inhibitor of activin receptor-like kinase 2 (ALK2) but is nonselective for highly homologous ALK3 and shows only modest kinome selectivity. Herein, we describe the discovery of a novel series of potent and selective ALK2 inhibitors by replacing th...

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Gepubliceerd in:Bioorg Med Chem Lett
Hoofdauteurs: Jiang, Jian-kang, Huang, Xiuli, Shamim, Khalida, Patel, Paresma R., Lee, Arthur, Wang, Amy Q., Nguyen, Kimloan, Tawa, Gregory, Cuny, Gregory D., Yu, Paul B., Zheng, Wei, Xu, Xin, Sanderson, Philip, Huang, Wenwei
Formaat: Artigo
Taal:Inglês
Gepubliceerd in: 2018
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Article
Online toegang:https://ncbi.nlm.nih.gov/pmc/articles/PMC6218249/
https://ncbi.nlm.nih.gov/pubmed/30227946
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2018.09.006
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