Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595941 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
Abstract
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.
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Organic Chemistry
Authors
Laurent Gavara, Virginie Suchaud, Lionel Nauton, Vincent Théry, Fabrice Anizon, Pascale Moreau,