6,7-二甲氧基-4-哌嗪喹唑啉缩氨基硫脲衍生物的合成及体外抗肿瘤活性研究  

Synthesis and in vitro Antitumor Activities of 6,7-Dimethoxy-4-piperazinquinazoline Thiosemicarbazone Derivatives

作　　者：刘海彬[1] 徐惠娟[1] 吕萍[1] 潘宁宁[1] 李双奇[1] 

机构地区：[1]辽宁科技学院生物医药与化学工程学院,本溪117004

出　　处：《化学学报》2012年第5期674-678,共5页Acta Chimica Sinica

基　　金：辽宁省教育厅科研项目(No.L2010204);辽宁省高等学校优秀人才支持计划(No.LJQ2011130);辽宁科技学院博士启动金(No.0906B1)资助项目~~

摘　　要：以4,5-二甲氧基-2-氨基苯甲酸和醋酸甲眯为起始原料,经环化、氯化、取代和缩合四步反应,设计、合成了六个未见文献报道的含有缩氨基硫脲的喹唑啉衍生物4a～4f,其结构用1H NMR,13C NMR,ESI-MS,IR及元素分析测试技术进行了表征.采用MTT法测试了化合物4a～4f对人胃癌SGC-7901、人口腔表皮样癌KB和人纤维肉瘤HT-1080的体外抗肿瘤活性.初步的测试结果表明,化合物4a和4f对HT1080表现出显著的抗肿瘤活性.Six new quinazoline derivatives 4a-4f bearing thiosemicabazone have been designed and syn- thesized by four step reactions of cyclization, chlorination, substitution and condensation using 2-amino-4,5-dimethoxybenzoic acid and methanimidamide acetate as starting materials. Their structures were confirmed by 1H NMR, 13C NMR, ESI-MS, IR techniques and elemental analysis. The in vitro antitu- mor activities of compounds 4a^4f against SGC-7901 （human gastric cancer）, KB （human oral epidermoid cancer） and HT-1080 （human fibrosarcoma） cell lines were tested using colorimetric MTT assay. The preliminary results indicated that compounds 4a and 4f showed significant antitumor activity against HT1080.

关 键 词：喹唑啉 缩氨基硫脲 抗肿瘤活性 MTT法 

分 类 号：R965[医药卫生—药理学] TQ460.1[医药卫生—药学]