Citation: Meng Yaqi, Li Erdong, Zhang Yang, Liu Shuan, Bao Chongnan, Yang Peng, Zhang Luye, Zhang Danqing, Wang Jikuan, Chen Yaxin, Li Na, Xin Jingchao, Zhao Peirong, Ke Yu, Zhang Qiurong, Liu Hongmin. Synthesis and Antitumor Activity Evaluation of 2, 4-Substituted Py-rimidine Derivatives Containing Trifluoromethyl[J]. Chinese Journal of Organic Chemistry, ;2019, 39(9): 2541-2548. doi: 10.6023/cjoc201903022 shu

Synthesis and Antitumor Activity Evaluation of 2, 4-Substituted Py-rimidine Derivatives Containing Trifluoromethyl

Meng Yaqi ^a,b ,
Li Erdong ^a,b ,
Zhang Yang ^a,b ,
Liu Shuan ^a,b ,
Bao Chongnan ^a,b ,
Yang Peng ^a,b ,
Zhang Luye ^a,b ,
Zhang Danqing ^a,b ,
Wang Jikuan ^a,b ,
Chen Yaxin ^a,b ,
Li Na ^a,b ,
Xin Jingchao ^a,b ,
Zhao Peirong ^a,b ,
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 Safety Evaluation, Zhengzhou 450001

Corresponding author: Ke Yu, ky@zzu.edu.cn Zhang Qiurong, zqr406@sina.com Liu Hongmin, liuhm@zzu.edu.cn
Received Date: 13 March 2019
Revised Date: 16 April 2019
Available Online: 26 September 2019
Fund Project: the National Natural Science Foundation of China 81430085Project supported by the National Natural Science Foundation of China (No. 81430085) and the Natural Science Foundation of Henan Province (No. 182300410321)the Natural Science Foundation of Henan Province 182300410321

Figures(2)

In order to find more effective antitumor drugs, a series of novel 2, 4-substituted pyrimidine derivatives containing trifluoromethyl were designed, synthesized, and evaluated for antitumor activity aganist EC-109 (human esophageal cancer cell), MGC-803 (human gastric cancer cell), PC-3 (human prostate cancer cell) and HepG-2 (human liver cancer cell). The results showed that some compounds displayed moderate to potent antitumor activity against PC-3. Among them, 2-(((4-((1-methyl-1H-tetrazol-5-yl)thio)-6-(trifluoromethyl)pyrimidin-2-yl)thio)methyl)benzo[d]thiazole (13w) possesses strong antitu-mor activity against PC-3 with IC₅₀ value of 1.76 μmol·L^-1, and the antitumor activity is significantly better than the positive control drug of 5-fluorouracil.
- trifluoromethyl,
- 2, 4-substituted pyrimidine derivatives,
- antitumor activity
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