کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1369641 | 981784 | 2012 | 4 صفحه PDF | دانلود رایگان |
β-Carboline family of compounds is a large group of alkaloids widely distributed in nature and exhibits broad-spectrum anti-tumor activities. We designed and synthesized two series of novel 1-carboxamide- and 6-sulfonamide-substituted β-carboline derivatives 7a–p and 12a–b, and their wild type B-Raf kinase inhibitory activities were described. Most compounds showed moderate to excellent inhibitory activities. Among them, 1-carboxamide-6-(N-(3-(dimethylamino)propyl)-sulfamoyl)-β-carboline, 7e exhibited potent activity (IC50 = 1.62 μM), showing the potential for further investigation as a lead compound.
Two series of novel 1-carboxamide and 6-sulfonamide substituted β-carboline derivatives 7a–o, 12a–b were designed and synthesized and their wild type B-Raf kinase inhibitory activities were described. Compound 1-carboxamide-6-(N-(3-(dimethylamino)propyl)sulfamoyl)-β-carboline, 7e exhibited potent activity (IC50 = 1.62 μM), showing the potential for further investigation as a lead compound.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 14, 15 July 2012, Pages 4783–4786