Synthesis, Cytotoxic Activity Evaluation of Novel 1,2,3-Triazole Linked Quinazoline Derivatives

被引：18
|
作者：
Song, Panpan [1 ,2 ,3 ,4 ]
Cui, Fei [1 ,2 ,3 ,4 ]
Li, Na [1 ,2 ,3 ,4 ]
Xin, Jingchao [1 ,2 ,3 ,4 ]
Ma, Qisheng [1 ,2 ,3 ,4 ]
Meng, Xiangchuan [1 ,2 ,3 ,4 ]
Wang, Chaojie [1 ,2 ,3 ,4 ]
Cao, Qinpo [1 ,2 ,3 ,4 ]
Gu, Yifei [1 ,2 ,3 ,4 ]
Ke, Yu [1 ,2 ,3 ,4 ]
Zhang, Qiurong [1 ,2 ,3 ,4 ]
Liu, Hongmin [1 ,2 ,3 ,4 ]
机构：
[1] Zhengzhou Univ, Sch Pharmaceut Sci, Zhengzhou 450001, Henan, Peoples R China
[2] Collaborat Innovat Ctr New Drug Res & Safety Eval, Zhengzhou 450001, Henan, Peoples R China
[3] Key Lab Henan Prov Drug Qual & Evaluat, Zhengzhou 450001, Henan, Peoples R China
[4] Zhengzhou Univ, Minist Educ, Key Lab Technol Drug Preparat, Zhengzhou 450001, Henan, Peoples R China
来源：
CHINESE JOURNAL OF CHEMISTRY | 2017年 / 35卷 / 10期
基金：
中国国家自然科学基金;
关键词：
quinazoline; triazole; synthesis; cytotoxicity; VITRO ANTITUMOR-ACTIVITY; BIOLOGICAL EVALUATION; ANTIPROLIFERATIVE ACTIVITY; ANTIFUNGAL ACTIVITY; CANCER-CELLS; INHIBITORS; ANALOGS; DESIGN; ANTICANCER; AGENTS;
D O I：
10.1002/cjoc.201700005
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
A series of novel 1,2,3-triazole-quinazoline derivatives were synthesized in five steps starting from anthranilamide by conventional methods. All the title compounds 10a-10r were evaluated for cytotoxic activity against four human cancer cell lines (MGC-803, EC-109, MCF-7 and HGC-27) using MTT assay in vitro. Some of the synthesized compounds exhibited moderate to potent activity against tested cancer cell lines. Among them, compounds 10 h and 10q exhibited excellent growth inhibition against HGC-27 and compound 10 m also possessed excellent activity against MCF-7, with IC50 values less than 1 mu mol/L. Especially, compound 10 h was more cytotoxic than 5-fluorouracil against all tested four human cancer cell lines.
引用
收藏
页码：1633 / 1639
页数：7
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