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 analogs 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.

中文翻译：

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糖基化吡咯K252c类似物的合成和抗增殖评价

星形孢菌素糖苷配基K252c的吡唑类似物最近被描述为三种Pim蛋白激酶同工型的有效抑制剂。为了评估糖部分的引入对该杂环支架的生物学活性的影响，合成了K252c的四个新的葡糖基化的吡唑类似物。他们的生物学评估表明，大多数活性化合物11和19在N12或N13位置被β- d-葡萄糖基部分取代，表现出对HCT116细胞的抗增殖活性。