Citation: 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]. Chinese Journal of Organic Chemistry, ;2019, 39(9): 2507-2514. doi: 10.6023/cjoc201902033 shu

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

Corresponding author: Fang Meijuan, fangmj@xmu.edu.cn Zhao Shengxian, 2086488660@qq.com
Received Date: 27 February 2019
Revised Date: 10 April 2019
Available Online: 10 September 2019
Fund Project: Project supported by the General Research Projects of Zhejiang Provincial Department of Education (No. Y201941989)the General Research Projects of Zhejiang Provincial Department of Education Y201941989

Figures(4)

A series of 4-substitued-1-(2-methyl-6-(pyridin-3-yl)-nicotinoyl) semicarbazides were synthesized 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.
- semicarbazides,
- bipyridine,
- molecular hybridization,
- biological activity
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