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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

刘海彬*,吕萍,潘宁宁,王文忠,王强   

  1. (辽宁科技学院生物医药与化学工程学院 本溪 117004)
  • 收稿日期:2011-11-01 修回日期:2012-03-09 出版日期:2012-09-10 发布日期:2012-09-10
  • 通讯作者: 刘海彬，讲师; Tel:0414-5861231; Fax:0414-4836532; E-mail:haibin0616@163.com; 研究方向：药物合成及不对称催化

Synthesis and in vitro Antitumor Activity of 6-Chloro-4-piperazinquinazolinethiosemicarbazone Derivatives

LIU Haibin*, LV Ping, PAN Ningning, WANG Wenzhong, WANG Qiang   

  1. (School of Biomedicine & Chemical Engineering,Liaoning Institute of Science and Technology,Benxi 117004,China)
  • Received:2011-11-01 Revised:2012-03-09 Published:2012-09-10 Online:2012-09-10

PDF

1296

被引次数

6 | 2

摘要： 以5-氯-2-氨基苯甲酸和甲酰胺为起始原料，经环化、氯化、取代和缩合反应，合成了3个未见文献报道的含哌嗪的喹唑啉衍生物5a~5c。 其结构用1H NMR、13C NMR、ESI-MS及IR测试技术进行了表征。 采用MTT法测试了化合物5a~5c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。 结果表明，化合物5a~5c对人胃癌SGC-7901和人纤维肉瘤HT-1080有弱的抑制活性，而对人口腔表皮样癌KB无明显抑制活性。

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

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 fibrosarcoma) cell lines of compounds 5a~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.

Key words: chloropiperazinquinazoline N-thiosemicarbazone substituted derivatives, antitumor activity, MTT assay,synthesis

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