Identification of pyrrolo[2,3-g]indazoles as new Pim kinase inhibitors

详细信息    查看全文

• 作者：Laurent Gavara ; Virginie Suchaud ; Lionel Nauton ; Vincent Thé ; ry ; Fabrice Anizonp> ; p>p>Fabrice.ANIZON@univ-bpclermont.frp> ; Pascale Moreau
• 关键词：Pyrrolo[2 ; 3-g]indazole ; Indazole ; Indole ; Pim kinase inhibition
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2013
• 出版时间：15 April, 2013
• 年：2013
• 卷：23
• 期：8
• 页码：2298-2301
• 全文大小：500 K

文摘

The synthesis and Pim kinase inhibition potency of a new series of pyrrolo[2,3-g]indazole derivatives is described. The results obtained in this preliminary structure-activity relationship study pointed out that sub-micromolar Pim-1 and Pim-3 inhibitory potencies could be obtained in this series, more particularly for compounds 10 and 20, showing that pyrrolo[2,3-g]indazole scaffold could be used for the development of new potent Pim kinase inhibitors. Molecular modeling experiments were also performed to study the binding mode of these compounds in Pim-3 ATP-binding pocket.