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Discovery of N-substituted 7-azaindoles as Pan-PIM kinases inhibitors - Lead optimization - Part III.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-12-10 , DOI: 10.1016/j.bmcl.2018.12.015 Claude Barberis 1 , James Pribish 1 , Elina Tserlin 1 , Alexandre Gross 1 , Mark Czekaj 1 , Matthieu Barragué 1 , Paul Erdman 1 , Sachin Maniar 1 , John Jiang 1 , Luke Fire 1 , Vinod Patel 1 , Andrew Hebert 2 , Mikhail Levit 2 , Anlai Wang 3 , Frank Sun 4 , Shih-Min A Huang 3
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-12-10 , DOI: 10.1016/j.bmcl.2018.12.015 Claude Barberis 1 , James Pribish 1 , Elina Tserlin 1 , Alexandre Gross 1 , Mark Czekaj 1 , Matthieu Barragué 1 , Paul Erdman 1 , Sachin Maniar 1 , John Jiang 1 , Luke Fire 1 , Vinod Patel 1 , Andrew Hebert 2 , Mikhail Levit 2 , Anlai Wang 3 , Frank Sun 4 , Shih-Min A Huang 3
Affiliation
N-substituted azaindoles were discovered as promising pan-PIM inhibitors. Lead optimization is described en route toward the identification of a clinical candidate. Modulation of physico-chemical properties allowed to solve inherent hERG and permeability liabilities. Compound 17 showed tumor growth inhibition in a KG1 tumor-bearing mouse model.
中文翻译：
N-取代的7-氮杂吲哚作为Pan-PIM激酶抑制剂的发现-铅优化-第三部分。
发现N-取代的吲哚吲哚是有希望的泛PIM抑制剂。在确定临床候选者的过程中描述了线索优化。理化性质的调节允许解决固有的hERG和渗透性负债。在具有KG1肿瘤的小鼠模型中，化合物17显示出肿瘤生长抑制作用。
更新日期：2018-12-10
中文翻译：
N-取代的7-氮杂吲哚作为Pan-PIM激酶抑制剂的发现-铅优化-第三部分。
发现N-取代的吲哚吲哚是有希望的泛PIM抑制剂。在确定临床候选者的过程中描述了线索优化。理化性质的调节允许解决固有的hERG和渗透性负债。在具有KG1肿瘤的小鼠模型中，化合物17显示出肿瘤生长抑制作用。
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