Acta Chimica Sinica ›› 2012, Vol. 0 ›› Issue (05): 674-678 .DOI: 10.6023/A1108171 Previous Articles     Next Articles



刘海彬, 徐惠娟, 吕萍, 潘宁宁, 李双奇   

  1. 辽宁科技学院生物医药与化学工程学院 本溪 117004
  • 投稿日期:2011-08-17 修回日期:2011-11-28 发布日期:2011-11-29
  • 通讯作者: 刘海彬
  • 基金资助:

    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.

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

Liu Haibin, Xu Huijuan, L? Ping, Pan Ningning, Li Shuangqi   

  1. School of Biomedical & Chemical Engineering, Liaoning Institute of Science and Technology, Benxi 117004
  • Received:2011-08-17 Revised:2011-11-28 Published:2011-11-29
  • Supported by:

    Project was supported by the Program of Liaoning Provincial Committee of Education (No. L2010204), the Program for Liaoning Excellent Talents in University (No. LJQ2011130) and the Ph. D. Program Foundation of Liaoning Institute of Science and Technology (No. 0906B1).

Six new quinazoline derivatives 4a~4f bearing thiosemicabazone have been designed and synthesized 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 antitumor 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.

Key words: quinazoline, thiosemicarbazone, antitumor activity, MTT assay