Identification of 1,6-dihydropyrazolo[4,3-c]carbazoles and 3,6-dihydropyrazolo[3,4-c]carbazoles as new Pim kinase inhibitors |
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Authors: | Virginie Suchaud Laurent Gavara Emmanuelle Saugues Lionel Nauton Vincent Théry Fabrice Anizon Pascale Moreau |
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Affiliation: | Clermont Université, Université Blaise Pascal, Institut de Chimie de Clermont-Ferrand, BP 10448, 63000 Clermont-Ferrand, France;CNRS, UMR 6296, ICCF, BP 80026, 63171 Aubière, France |
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Abstract: | New 1,6-dihydropyrazolo[4,3-c]carbazoles and 3,6-dihydropyrazolo[3,4-c]carbazoles were prepared and evaluated for their Pim kinase inhibitory potencies as well as their antiproliferative activities toward two prostatic cancer cell lines. Pyrazolocarbazole 15a was found to be a potent Pim kinase modulator with inhibitory potency toward the three isoforms. Compound 6c strongly inhibited Pim-3 with weaker effect toward Pim-1 and Pim-2, and thus could be used as an interesting molecular tool to study Pim-3 biological functions. |
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Keywords: | Pyrazolocarbazoles Kinase inhibitors Pim kinases In vitro antiproliferative activities |
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