Synthesis and biological evaluation of the pirfenidone derivatives as antifibrotic agents

…, Y Pan, W Huang, Y Yang, Z Wang, Q Li, Y Zhao…

Index: Ma, Zhen; Pan, Youlu; Huang, Wenhai; Yang, Yewei; Wang, Zunyuan; Li, Qin; Zhao, Yin; Zhang, Xinyue; Shen, Zhengrong Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 1 p. 220 - 223

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Citation Number: 7

Abstract

Abstract A total of 24 pirfenidone derivatives were designed, synthesized and evaluated for their inhibitory activity against the human lung fibroblast cell line MRC-5. These compounds showed the remarkable proliferation inhibition against MRC-5 compared to pirfenidone as the positive control. The possible mechanism of this kind of derivatives as antifibrotic agents was explored. The molecular docking and p38 binding affinity assays demonstrated that ...