2. Academic Validation
  3. Discovery and evaluation of 3,5-disubstituted indole derivatives as Pim kinase inhibitors

Discovery and evaluation of 3,5-disubstituted indole derivatives as Pim kinase inhibitors

  • Bioorg Med Chem Lett. 2018 Aug 1;28(14):2513-2517. doi: 10.1016/j.bmcl.2018.05.054.
Kunal N More 1,  Victor S Hong 1,  Ahyeon Lee 1,  Jongsung Park 1,  Shin Kim 2,  Jinho Lee 3
Affiliations

Affiliations

  • 1 Department of Chemistry, Keimyung University, Daegu 42601, Republic of Korea.
  • 2 Department of Immunology, School of Medicine, Keimyung University, Daegu 42601, Republic of Korea. Electronic address: [email protected].
  • 3 Department of Chemistry, Keimyung University, Daegu 42601, Republic of Korea. Electronic address: [email protected].
PMID: 29871845 DOI: 10.1016/j.bmcl.2018.05.054
Abstract

Pim kinases are promising therapeutic targets for the treatment of hematological cancers. A potent Pim kinase inhibitor 7f, 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 compound 43 with improved cellular potency and high selectivity against a panel of 14 different kinases.

Keywords

Indole; Inhibitor; MV4-11; Pim-1; Pim-2; Pim-3.

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