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

doi:10.6023/cjoc201903022

Chin. J. Org. Chem. ›› 2019, Vol. 39 ›› Issue (9): 2541-2548.DOI: 10.6023/cjoc201903022 Previous Articles Next Articles

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含三氟甲基的2,4-取代嘧啶衍生物的合成及抗肿瘤活性评价

孟娅琪^a,b, 李二冬^a,b, 张洋^a,b, 刘栓^a,b, 包崇男^a,b, 杨鹏^a,b, 张路野^a,b, 张丹青^a,b, 王继宽^a,b, 陈雅欣^a,b, 栗娜^a,b, 辛景超^a,b, 赵培荣^a,b, 可钰^a,b, 张秋荣^a,b, 刘宏民^a,b

a 郑州大学药学院郑州 450001;
b 新药创制与药物安全性评价河南省协同创新中心郑州 450001

收稿日期:2019-03-13 修回日期:2019-04-16 发布日期:2019-04-26
通讯作者: 可钰, 张秋荣, 刘宏民 E-mail:ky@zzu.edu.cn;zqr406@sina.com;liuhm@zzu.edu.cn
基金资助:
国家自然科学基金（No.81430085）、河南省自然科学基金（No.182300410321）资助项目.

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

Received:2019-03-13 Revised:2019-04-16 Published:2019-04-26
Contact: 10.6023/cjoc201903022 E-mail:ky@zzu.edu.cn;zqr406@sina.com;liuhm@zzu.edu.cn
Supported by:
Project supported by the National Natural Science Foundation of China (No. 81430085) and the Natural Science Foundation of Henan Province (No. 182300410321).

1. Synthesis and Antitumor Activity Evaluation of 2,4-Substituted Py-rimidine Derivatives Containing Trifluoromethyl.PDF(1800KB)

Abstract

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.

Key words: trifluoromethyl, 2,4-substituted pyrimidine derivatives, antitumor activity

Cite this article

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]. Chin. J. Org. Chem., 2019, 39(9): 2541-2548.

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含三氟甲基的2,4-取代嘧啶衍生物的合成及抗肿瘤活性评价

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

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