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Article Dans Une Revue Bioorganic and Medicinal Chemistry Letters Année : 2012

Kinase inhibitory potencies and in vitro antiproliferative activities of N-10 substituted pyrrolo[2,3-a] carbazole derivatives

Résumé

Development of potent and selective Pim kinase inhibitors has recently emerged as an important field for the design of new anti-cancer drugs. We report the synthesis of new N-10-substituted pyrrolo[2,3-a]carbazole derivatives and their evaluation as Pim kinase inhibitors. Moreover, in vitro antiproliferative activity of these compounds was evaluated toward a human fibroblast primary culture and three human solid cancer cell lines (PA1, PC3 and DU145). Compounds 3, 7 and 10 showed inhibitory potencies toward Pim- 1 and Pim-3 in the nanomolar range. Additionally, dimethylamino analog 10 also demonstrated interesting sub-micromolar antiproliferative activities toward the cell lines tested.
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Dates et versions

hal-00711767 , version 1 (25-06-2012)

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  • HAL Id : hal-00711767 , version 1

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Rufine Akué-Gédu, Boris Letribot, Emmanuelle Saugues, Eric Debiton, Fabrice Anizon, et al.. Kinase inhibitory potencies and in vitro antiproliferative activities of N-10 substituted pyrrolo[2,3-a] carbazole derivatives. Bioorganic and Medicinal Chemistry Letters, 2012, 22, pp.3807-3809. ⟨hal-00711767⟩
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