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Pan-PIM激酶抑制剂SARxxxx92的发现对KG1肿瘤模型有效
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2020-10-20 , DOI: 10.1016/j.bmcl.2020.127625 Claude Barberis 1 , Paul Erdman 2 , Mark Czekaj 1 , Luke Fire 3 , James Pribish 1 , Elina Tserlin 4 , Sachin Maniar 1 , Joseph D Batchelor 1 , Jinyu Liu 1 , Vinod F Patel 5 , Andrew Hebert 6 , Mikhail Levit 6 , Anlai Wang 7 , Frank Sun 8 , Shih-Min A Huang 9
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更新日期：2020-10-30
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2020-10-20 , DOI: 10.1016/j.bmcl.2020.127625 Claude Barberis 1 , Paul Erdman 2 , Mark Czekaj 1 , Luke Fire 3 , James Pribish 1 , Elina Tserlin 4 , Sachin Maniar 1 , Joseph D Batchelor 1 , Jinyu Liu 1 , Vinod F Patel 5 , Andrew Hebert 6 , Mikhail Levit 6 , Anlai Wang 7 , Frank Sun 8 , Shih-Min A Huang 9
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发现N-取代的氮吲哚是有效的泛PIM抑制剂。铅的优化，以结构为指导并着重于理化性质，使我们能够解决固有的hERG和通透性负债，并提供了化合物27，其随后影响了小鼠模型中KG-1肿瘤的生长。
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