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Synthesis and antiproliferative evaluation of glucosylated pyrazole analogs of K252c |
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| Authors: | Bachir Douara Yannick J Esvan Elisabeth Pereira Francis Giraud Yulia L Volodina Dmitry N Kaluzhny Alexander A Shtil Fabrice Anizon Pascale Moreau |
| Institution: | 1. Université Clermont Auvergne, CNRS, ICCF, F-63000 Clermont-Ferrand, France;2. Laboratoire de Phytochimie et de Pharmacologie, Département de Chimie, Faculté des Sciences Exactes et Informatique, Université Mohamed Seddik Ben Yahia, 18000 Jijel, Algeria;3. Blokhin National Medical Center of Oncology, 115478 Moscow, Russian Federation;4. Engelhardt Institute of Molecular Biology, 119991 Moscow, Russian Federation;5. ITMO University, 197101 Saint-Petersburg, Russian Federation |
| 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 compounds 11 and 19 substituted by a β-d-glucosyl moiety at N12 or N13 positions exhibited antiproliferative activities toward HCT116 cells. |
| Keywords: | Indolocarbazole K252c analogs Glucosylated derivatives Antiproliferative activity |
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