Synthesis, structure, and biological assay of cinnamic amides as potential EGFR kinase inhibitors

M Zhang, X Lu, HJ Zhang, N Li, Y Xiao, HL Zhu…

Index: Zhang, Mao; Lu, Xiang; Zhang, Hong-Jia; Li, Na; Xiao, Yu; Zhu, Hai-Liang; Ye, Yong-Hao Medicinal Chemistry Research, 2013 ,  vol. 22,  # 2  p. 986 - 994

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Citation Number: 4

Abstract

Abstract A series of derivatives of cinnamic amide (compounds 2a–2v) were synthesized and evaluated for antiproliferative activities against the human breast cancer cell line MCF-7- and EGFR-inhibitory activities. The structures of compounds 2b and 2i were determined by single-crystal X-ray diffraction analysis. Compounds 2f and 2j showed moderate EGFR inhibitory activity with IC 50 values of 5.16 and 7.37 μM, respectively. Docking simulation ...