Discovery of N-substituted 7-azaindoles as Pan-PIM kinase inhibitors - Lead series identification - Part II.

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. Copyright © 2017 Elsevier Ltd. All rights reserved.

Citation

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. Discovery of N-substituted 7-azaindoles as Pan-PIM kinase inhibitors - Lead series identification - Part II. Bioorganic & medicinal chemistry letters. 2017 Oct 15;27(20):4735-4740

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PMID: 28927793

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