Citation: Song Panpan, Li Na, Cui Fei, Xin Jingchao, Zhang Xiaosong, Cao Qinpo, Wang Chaojie, Dai Wenjie, Meng Xiangchuan, Liu Meng, Chang Tonghang, Liu Qingyi, Sun Yuehonga, Ke Yu, Zhang Qiurong, Liu Hongmin. Synthesis and Antitumor Activity Evaluation of 2, 4, 6-Trisubstituted Pyrimidine Derivatives[J]. Chinese Journal of Organic Chemistry, ;2017, 37(10): 2725-2735. doi: 10.6023/cjoc201705013 shu

Synthesis and Antitumor Activity Evaluation of 2, 4, 6-Trisubstituted Pyrimidine Derivatives

Song Panpan ^a,b ,
Li Na ^a,b ,
Cui Fei ^a,b ,
Xin Jingchao ^a,b ,
Zhang Xiaosong ^a,b ,
Cao Qinpo ^a,b ,
Wang Chaojie ^a,b ,
Dai Wenjie ^a ,
Meng Xiangchuan ^a ,
Liu Meng ^a ,
Chang Tonghang ^a ,
Liu Qingyi ^a ,
Sun Yuehonga ^a ,
Ke Yu ^a,b,, ,
Zhang Qiurong ^a,b,, ,
Liu Hongmin ^a,b,,

a.
School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001
b.
Collaborative Innovation Center of New Drug Research and Saftry Evaluation, Zhengzhou 450001

Corresponding author: Ke Yu, ky@zzu.edu.cn Zhang Qiurong, zqr406@sina.com Liu Hongmin, liuhm@zzu.edu.cn
Received Date: 8 May 2017
Revised Date: 23 May 2017
Available Online: 7 October 2017
Fund Project: Project supported by the National Natural Science Foundation of China (No. 81430085) and the Research Project of Science and Technology Bureau of Zhengzhou City (No.141PQYJS554)the Research Project of Science and Technology Bureau of Zhengzhou City No.141PQYJS554the National Natural Science Foundation of China 81430085

Figures(3)

With the aim of obtaining potential antitumor candidates with more efficiency and more economic value. 40 2, 4, 6-trisubstituted pyrimidine derivatives bearing chalcone moiety were synthesized via cyclization, chlorination, substitution with benzoylacetate and ethylacetoacetate as the starting materials. The structures of target products were confirmed by ¹H NMR, ^I3C NMR and HRMS. 2, 4, 6-Trisubstituted pyrimidine derivatives bearing chalcone moiety were evaluated for anticancer activity on four human cancer cell lines including EC-109, MGC-803, HepG-2 and MDA-MB-231 by CCK-8 (cell counting Kit-8) assay. Among them, (E)-1-(4-((2-(((1H-benzo[d]imidazol-2-yl)methyl)thio)-6-methylpyrimidin-4-yl)amino)-phe-nyl)-3-(3, 4, 5-trimethoxyphenyl)prop-2-en-1-one (13u) were more cytotoxic against MGC-803 and MDA-MB-231 cell lines, with IC₅₀ values of 0.99 and 1.77 μmol·L^-1, respectively.
- 2, 4, 6-trisubstituted pyrimidine,
- chalcone,
- antitumor
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