应用化学2012，Vol.29Issue(9)：1000-1005,6.DOI:10.3724/SP.J.1095.2012.00481
6-氯-4-哌嗪基喹唑啉缩氨基硫脲类化合物的合成及体外抗肿瘤活性
Synthesis and in vitro Antitumor Activity of 6-Chloro-4-piperazinquinazolinethiosemicarbazone Derivatives
摘要
Abstract
Three new quinazoline derivatives 5a ~5c bearing piperazine have been designed and synthesized by four-step reactions of cyclization, chlorination, substitution and condensation using 2-amino-5-chlorobenzoic acid and formamide as starting materials. Their structures were confirmed by 1H NMR, 13C NMR, ESI-MS and IR. The in vitro cytotoxicities against SGC-7901 (human gastric cancer) , KB ( human oral epidermoid cancer) and HT-1080 ( human fibrosareoma) cell lines of compounds Sa - 5c were tested with colorimetric MTT assay. The results indicated that compounds 5a ~5c had poor anticancer activities against SGC-7901 and HT-1080 cell lines, while had no notable inhibitory activity against KB cell lines.关键词
氯哌嗪喹唑啉N-缩氨基硫脲取代衍生物/抗肿瘤活性/MTT法/合成Key words
chloropiperazinquinazoline N-thiosemicarbazone substituted derivatives, antitumor activity, MTT assay, synthesis分类
化学化工引用本文复制引用
刘海彬,吕萍,潘宁宁,王文忠,王强..6-氯-4-哌嗪基喹唑啉缩氨基硫脲类化合物的合成及体外抗肿瘤活性[J].应用化学,2012,29(9):1000-1005,6.基金项目
辽宁省教育厅科研项目(L2010204),辽宁省高等学校优秀人才支持计划资助(LJQ2011130),辽宁科技学院博士启动金项目(0906B1) （L2010204）
