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Identification of 1,6-dihydropyrazolo[4,3-c]carbazoles and 3,6-dihydropyrazolo[3,4-c]carbazoles as new Pim kinase inhibitors
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2013-05-16 , DOI: 10.1016/j.bmc.2013.05.011 Virginie Suchaud , Laurent Gavara , Emmanuelle Saugues , Lionel Nauton , Vincent Théry , Fabrice Anizon , Pascale Moreau
中文翻译:
鉴定1,6-二氢吡唑并[4,3- c ]咔唑和3,6-二氢吡唑并[3,4- c ]咔唑作为新的Pim激酶抑制剂
更新日期:2013-05-16
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2013-05-16 , DOI: 10.1016/j.bmc.2013.05.011 Virginie Suchaud , Laurent Gavara , Emmanuelle Saugues , Lionel Nauton , Vincent Théry , Fabrice Anizon , Pascale Moreau
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.
中文翻译:
鉴定1,6-二氢吡唑并[4,3- c ]咔唑和3,6-二氢吡唑并[3,4- c ]咔唑作为新的Pim激酶抑制剂
制备了新的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,并评估了它们对Pim激酶的抑制能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是有效的Pim激酶调节剂,对三种同工型具有抑制作用。化合物6c强烈抑制Pim-3,对Pim-1和Pim-2的作用较弱,因此可以用作研究Pim-3生物学功能的有趣分子工具。