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  • Title: Pim kinase inhibitory and antiproliferative activity of a novel series of meridianin C derivatives.
    Author: More KN, Jang HW, Hong VS, Lee J.
    Journal: Bioorg Med Chem Lett; 2014 Jun 01; 24(11):2424-8. PubMed ID: 24775304.
    Abstract:
    A novel series of meridianin C derivatives substituted at C-5 position were prepared. These derivatives were tested for their kinase inhibitory potencies against all three family members of the pim kinases (Pim-1, Pim-2 and Pim-3). In addition, their antiproliferative activity towards three human leukemia cell lines as MV4-11, Jurkat clone E6-1 and K562 has been evaluated. Structure activity relationships at C-3 and C-5 positions of indole were performed to better understand the mechanism behind the enhanced potency. Compound 7f, the most active compound of the series showed a single-digit nanomolar IC50 with selectivity towards Pim-1 kinase.
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