The synthesis and biological evaluation of some caffeic acid amide derivatives: E-2-Cyano-(3-substituted phenyl)acrylamides |
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| Authors: | Wei Zhou Hai-bo Li Chun-nian Xia Xian-ming Zheng Wei-xiao Hu |
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| Institution: | 1. College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou, 310014, PR China;2. Nantong Institute for the Control of Pharmaceutical and Biological Products, Nantong, Jiangsu 226001, PR China;3. Zhejiang Huafang Pharmaceutical Co., Ltd, Taizhou, Zhejiang 318020, PR China |
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| Abstract: | A series of caffeic acid amide derivatives 2-cyano-(3-substituted phenyl)acrylamides were synthesized via Knoevenogal condensation of substituted benzaldehydes with cyanoacetamides. The structure of compound 1f was determined as E-isomer by X-ray diffractive analysis. The biological screening tests in vitro showed that compound 1b has obvious inhibitory activities against human gastric carcinoma cell line BGC-823, human nasopharyngeal carcinoma cell line KB and human hepatoma cell line BEL-7402 with IC50 values of 5.6 μg/mL, 13.1 μg/mL and 12.5 μg/mL, respectively. Some preliminary structure–activity relationships (SAR) were also proposed which may provide a direction for further study. |
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