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

作　　者：Panpan Song Fei Cui Na Li Jingchao Xin Qisheng Ma Xiangchuan Meng Chaojie Wang Qinpo Cao Yifei Gu Yu Ke Qiurong Zhang Hongmin Liu 

机构地区：[1]School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, Henan 450001, China [2]Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou, Henan 450001, China [3]Key Laboratory of Henan Province for Drug Quality and Evaluation, Zhengzhou, Henan 450001, China [4]Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education, Zhengzhou, Henan 450001, China

出　　处：《Chinese Journal of Chemistry》2017年第10期1633-1639,共7页中国化学（英文版）

摘　　要：A series of novel 1,2,3-triazole-quinazoline derivatives were synthesized in five steps starting from anthranila- mide 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 synthe- sized compounds exhibited moderate to potent activity against tested cancer cell lines. Among them, compounds 10h and 10q exhibited excellent growth inhibition against HGC-27 and compound 10m also possessed excellent ac- tivity against MCF-7, with IC50 values less than 1 μmol/L. Especially, compound 10h was more cytotoxic than 5-fluorouracil against all tested four human cancer cell lines.A series of novel 1,2,3-triazole-quinazoline derivatives were synthesized in five steps starting from anthranila- mide 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 synthe- sized compounds exhibited moderate to potent activity against tested cancer cell lines. Among them, compounds 10h and 10q exhibited excellent growth inhibition against HGC-27 and compound 10m also possessed excellent ac- tivity against MCF-7, with IC50 values less than 1 μmol/L. Especially, compound 10h was more cytotoxic than 5-fluorouracil against all tested four human cancer cell lines.

关 键 词：QUINAZOLINE TRIAZOLE SYNTHESIS CYTOTOXICITY 

分 类 号：X503.231[环境科学与工程—环境工程] TS254.7[轻工技术与工程—水产品加工及贮藏工程]