Design, synthesis and biological evaluation of ¦Â-carboline derivatives as novel inhibitors targeting B-Raf kinase

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• 作者：Botao Xin ; Weifang Tang ; Yue Wang ; Guowu Lin ; Haichun Liu ; Yu Jiao ; Yong Zhu ; Haoliang Yuan ; Yadong Chen ; Tao Lu
• 关键词：B-Raf kinase inhibitor ; ¦Â-Carboline derivatives ; Kinase inhibitory activities
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 出版时间：15 July, 2012
• 年：2012
• 卷：22
• 期：14
• 页码：4783-4786
• 全文大小：510 K

文摘

¦Â-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 ¦Â-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)-¦Â-carboline, 7e exhibited potent activity (IC₅₀ = 1.62 ¦ÌM), showing the potential for further investigation as a lead compound.