Clermont Université, Université Blaise Pascal, Institut de Chimie de Clermont-Ferrand, BP 10448, 63000 Clermont-Ferrand, France.
Bioorg Med Chem. 2013 Jul 15;21(14):4102-11. doi: 10.1016/j.bmc.2013.05.011. Epub 2013 May 16.
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.
新的 1,6-二氢吡唑并[4,3-c]咔唑和 3,6-二氢吡唑并[3,4-c]咔唑被制备并评估了它们作为 Pim 激酶抑制剂的潜力以及对两种前列腺癌细胞系的抗增殖活性。发现吡唑并咔唑 15a 是一种有效的 Pim 激酶调节剂，对三种同工型均具有抑制作用。化合物 6c 强烈抑制 Pim-3，对 Pim-1 和 Pim-2 的作用较弱，因此可用作研究 Pim-3 生物学功能的有趣分子工具。
