Discovery of N-substituted 7-azaindoles as Pan-PIM kinase inhibitors – Lead series identification – Part II. Issue 20 (15th October 2017)

• Record Type: Journal Article
• Authors: Barberis, Claude; Moorcroft, Neil; Pribish, James; Tserlin, Elina; Gross, Alexandre; Czekaj, Mark; Barrague, Matthieu; Erdman, Paul; Majid, Tahir; Batchelor, Joseph; Levit, Mikhail; Hebert, Andrew; Shen, Liduo; Moreno-Mazza, Sandra; Wang, Anlai
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 20(2017)
• Page Start: 4735
• Page End: 4740
• Publication Date: 2017-10-15
• Subjects: Pan-PIM kinases -- X-ray crystallography -- AML -- PK/PD -- Hit-to-Lead -- Small molecule inhibitor -- Cancer; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.08.068
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: 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.