3 years ago

Synthesis and antiproliferative evaluation of glucosylated pyrazole analogues of K252c

Synthesis and antiproliferative evaluation of glucosylated pyrazole analogues of K252c
Pyrazole analogs of the staurosporine aglycon K252c were recently described as potent inhibitors of the three Pim protein kinase isoforms. To evaluate the impact of the introduction of a sugar moiety on the biological activities of this heterocyclic scaffold, four new glucosylated pyrazole analogues of K252c were synthesized. Their biological evaluation demonstrated that most active compounds 11 and 19 substituted by a β-d-glucosyl moiety at N12 or N13 positions exhibited antiproliferative activities toward HCT116 cells.

Publisher URL: www.sciencedirect.com/science

DOI: S0040402018300395

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