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

…, W Tang, Y Wang, G Lin, H Liu, Y Jiao, Y Zhu…

Index: Xin, Botao; Tang, Weifang; Wang, Yue; Lin, Guowu; Liu, Haichun; Jiao, Yu; Zhu, Yong; Yuan, Haoliang; Chen, Yadong; Lu, Tao Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 14 p. 4783 - 4786

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Citation Number: 12

Abstract

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- ...