首页 | 本学科首页   官方微博 | 高级检索  
     


Identification of 1,6-dihydropyrazolo[4,3-c]carbazoles and 3,6-dihydropyrazolo[3,4-c]carbazoles as new Pim kinase inhibitors
Authors:Virginie Suchaud  Laurent Gavara  Emmanuelle Saugues  Lionel Nauton  Vincent Théry  Fabrice Anizon  Pascale Moreau
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
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.
Keywords:Pyrazolocarbazoles  Kinase inhibitors  Pim kinases  In vitro antiproliferative activities
本文献已被 ScienceDirect 等数据库收录!
设为首页 | 免责声明 | 关于勤云 | 加入收藏

Copyright©北京勤云科技发展有限公司  京ICP备09084417号