Discovery and evaluation of 3, 5-disubstituted indole derivatives as Pim kinase inhibitors. Issue 14 (1st August 2018)

• Record Type: Journal Article
• Authors: More, Kunal N.; Hong, Victor S.; Lee, Ahyeon; Park, Jongsung; Kim, Shin; Lee, Jinho
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 28:Issue 14(2018)
• Page Start: 2513
• Page End: 2517
• Publication Date: 2018-08-01
• Subjects: Pim-1 -- Pim-2 -- Pim-3 -- Inhibitor -- Indole -- MV4-11; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2018.05.054
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Highlights: Pim-1 and Pim-3 kinase inhibitors were prepared using indole as the core structure. 2-Aminopyrimidine of meridianin C derivative was replaced by substituted benzene. Cellular potency of inhibitor was improved by the optimization process. Abstract: Pim kinases are promising therapeutic targets for the treatment of hematological cancers. A potent Pim kinase inhibitor7f, derived from meridianin C, was further optimized by the replacement of 2-aminopyrimidine with substituted benzene. The optimization of the C-3 and C-5 positions of indole yielded compound43 with improved cellular potency and high selectivity against a panel of 14 different kinases.