Synthesis and antiproliferative evaluation of glucosylated pyrazole analogs of K252c. Issue 8 (22nd February 2018)

• Record Type: Journal Article
• Authors: Douara, Bachir; Esvan, Yannick J.; Pereira, Elisabeth; Giraud, Francis; Volodina, Yulia L.; Kaluzhny, Dmitry N.; Shtil, Alexander A.; Anizon, Fabrice; Moreau, Pascale
• Is Part Of: Tetrahedron. Volume 74:Issue 8(2018)
• Page Start: 892
• Page End: 901
• Publication Date: 2018-02-22
• Subjects: Indolocarbazole -- K252c analogs -- Glucosylated derivatives -- Antiproliferative activity; Chemistry, Organic -- Periodicals; 547.005
• DOI: 10.1016/j.tet.2018.01.017
• Languages: English
• ISSNs: 0040-4020

Abstract

Abstract: 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 compounds11 and19 substituted by a β-d -glucosyl moiety at N12 or N13 positions exhibited antiproliferative activities toward HCT116 cells. Graphical abstract: