Synthesis and Biological Activity Research of 4-Substitued-1-(2-methyl-6-(pyridin-3-yl)-nicotinoyl) Semicarbazides

doi:10.6023/cjoc201902033

Chin. J. Org. Chem. ›› 2019, Vol. 39 ›› Issue (9): 2507-2514.DOI: 10.6023/cjoc201902033 Previous Articles Next Articles

ARTICLE

4-取代-1-(2-甲基-6-(吡啶-3-基)-烟酰)氨基脲类衍生物合成与生物活性研究

胡鸿雨^a, 吴俊^b, 袁建锋^a, 王珍妮^a, 李晨帆^a, 严晓阳^a, 方美娟^b, 赵胜贤^a,c

a 浙江师范大学行知学院金华 321004;
b 厦门大学药学院厦门 361102;
c 宁波大学科学技术学院慈溪 315302

收稿日期:2019-02-27 修回日期:2019-04-10 发布日期:2019-05-10
通讯作者: 方美娟, 赵胜贤 E-mail:fangmj@xmu.edu.cn;2086488660@qq.com
基金资助:
浙江省教育厅一般课题基金（No.Y201941989）资助项目.

Synthesis and Biological Activity Research of 4-Substitued-1-(2-methyl-6-(pyridin-3-yl)-nicotinoyl) Semicarbazides

Hu Hongyu^a, Wu Jun^b, Yuan Jianfeng^a, Wang Zhenni^a, Li Chenfan^a, Yan Xiaoyan^a, Fang Meijuan^b, Zhao Shengxian^a,c

a Xingzhi College, Zhejiang Normal University, Jinhua 321004;
b School of Pharmaceutical Sciences, Xiamen University, Xiamen 361102;
c College of Science and Technology, Ningbo University, Cixi 315302

Received:2019-02-27 Revised:2019-04-10 Published:2019-05-10
Contact: 10.6023/cjoc201902033 E-mail:fangmj@xmu.edu.cn;2086488660@qq.com
Supported by:
Project supported by the General Research Projects of Zhejiang Provincial Department of Education (No. Y201941989).

1. Synthesis and Biological Activity Research of 4-Substitued-1-(2-methyl-6-(pyridin-3-yl)-nicotinoyl) Semicarbazides.PDF(4873KB)

Abstract

A series of 4-substitued-1-(2-methyl-6-(pyridin-3-yl)-nicotinoyl) semicarbazides were synthesized[A3] via molecular hybridization strategy. The synthesized compounds were screened for their anticancer potential against different cancer cells viz human hepatocelular carcinoma (QGY-7703), non-small cell lung (NCl-H460) and human breast (MCF-7) cancer cell lines by methyl thiazolyl tetrazolium (MTT) assay. 1-(2-Methyl-6-(pyridin-3-yl)nicotinoyl)-4-(2,4,6-trichlorophenyl)semicarbazide (4n) showed significant anticancer activity in these cancer cell lines with a range of IC₅₀ values from 8.89 μmol/L to 11.45 μmol/L. Further biology studies showed that 4n treatment obviously increased the level of cleaved PARP and induced the apoptosis in QGY-7703 cells.

Key words: semicarbazides, bipyridine, molecular hybridization, biological activity

Cite this article

Hu Hongyu, Wu Jun, Yuan Jianfeng, Wang Zhenni, Li Chenfan, Yan Xiaoyan, Fang Meijuan, Zhao Shengxian. Synthesis and Biological Activity Research of 4-Substitued-1-(2-methyl-6-(pyridin-3-yl)-nicotinoyl) Semicarbazides[J]. Chin. J. Org. Chem., 2019, 39(9): 2507-2514.

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4-取代-1-(2-甲基-6-(吡啶-3-基)-烟酰)氨基脲类衍生物合成与生物活性研究

Synthesis and Biological Activity Research of 4-Substitued-1-(2-methyl-6-(pyridin-3-yl)-nicotinoyl) Semicarbazides

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