Discovery of 3-(4-sulfamoylnaphthyl)pyrazolo[1,5-a]pyrimidines as potent and selective ALK2 inhibitors.
Discovery of 3-(4-sulfamoylnaphthyl)pyrazolo[1,5-a]pyrimidines as potent and selective ALK2 inhibitors.
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DOI：
10.1016/j.bmcl.2018.09.006
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发表时间：
2018-11-01
影响因子：
2.7
通讯作者：
Huang W
中科院分区：
文献类型：
--
作者：
Jiang JK;Huang X;Shamim K;Patel PR;Lee A;Wang AQ;Nguyen K;Tawa G;Cuny GD;Yu PB;Zheng W;Xu X;Sanderson P;Huang W
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 the quinolinyl with a 4-(sulfamoyl)naphthyl, yielding ALK2 inhibitors that exhibit not only excellent discrimination versus ALK3 but also high kinome selectivity. In addition, the optimized compound 23 demonstrates good ADME and in vivo pharmacokinetic properties.
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影响因子：
9.8
作者：
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通讯作者：
Harris, Adrian L.
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影响因子：
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作者：
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DOI：
10.1002/jbmr.2820
发表时间：
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期刊：
Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research
影响因子：
--
作者：
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通讯作者：
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DOI：
10.1016/j.berh.2007.11.007
发表时间：
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影响因子：
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作者：
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7.3
作者：
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