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

被引：19

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

页码：1633 / 1639

页数：7

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