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Discovery of N-substituted 7-azaindoles as Pan-PIM kinase inhibitors – Lead series identification – Part II
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2017-09-09 , DOI: 10.1016/j.bmcl.2017.08.068
Claude Barberis , Neil Moorcroft , James Pribish , Elina Tserlin , Alexandre Gross , Mark Czekaj , Matthieu Barrague , Paul Erdman , Tahir Majid , Joseph Batchelor , Mikhail Levit , Andrew Hebert , Liduo Shen , Sandra Moreno-Mazza , Anlai Wang

N-Substituted azaindoles have been discovered as pan-PIM kinase inhibitors. Initial SAR, early ADME and PK/PD data of a series of compounds is described and led to the identification of promising pan-PIM inhibitors which validated our interest in the 7-azaindole scaffold and led us to pursue the identification of a clinical candidate.



中文翻译:

发现N-取代的7-氮杂吲哚作为Pan-PIM激酶抑制剂–铅系列鉴定–第二部分

已经发现N-取代的氮杂吲哚是泛-PIM激酶抑制剂。描述了一系列化合物的初始SAR,早期ADME和PK / PD数据,并导致鉴定出有前途的pan-PIM抑制剂,从而验证了我们对7-氮杂吲哚支架的兴趣,并促使我们进行临床候选物的鉴定。

更新日期:2017-09-09
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