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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- 作者：Virginie Suchaud ; Laurent Gavara ; Emmanuelle Saugues ; Lionel Nauton ; Vincent Thé ; ry ; Fabrice Anizon
- 关键词：Pyrazolocarbazoles ; Kinase inhibitors ; Pim kinases ; In vitro antiproliferative activities
- 刊名：Bioorganic and Medicinal Chemistry
- 出版年：2013
- 出版时间：15 July, 2013
- 年：2013
- 卷：21
- 期：14
- 页码：4102-4111
- 全文大小：953 K
文摘
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.