Discovery of N-substituted 7-azaindoles as Pan-PIM kinases inhibitors – Lead optimization – Part III. Issue 3 (1st February 2019)

• Record Type: Journal Article
• Authors: Barberis, Claude; Pribish, James; Tserlin, Elina; Gross, Alexandre; Czekaj, Mark; Barragué, Matthieu; Erdman, Paul; Maniar, Sachin; Jiang, John; Fire, Luke; Patel, Vinod; Hebert, Andrew; Levit, Mikhail; Wang, Anlai; Sun, Frank; Huang, Shih-Min A.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 29:Issue 3(2019)
• Page Start: 491
• Page End: 495
• Publication Date: 2019-02-01
• Subjects: Lead -- Pan-PIM kinases -- AML -- PK/PD -- Tumor growth inhibition -- Cancer; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2018.12.015
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: 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.