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

doi:10.6023/A1108171

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

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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

刘海彬, 徐惠娟, 吕萍, 潘宁宁, 李双奇

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 E-mail:haibin0616@163.com
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

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

Cite this article

Liu Haibin, Xu Huijuan, L? Ping, Pan Ningning, Li Shuangqi. Synthesis and in vitro Antitumor Activities of 6,7-Dimethoxy-4-piperazinquinazoline Thiosemicarbazone Derivatives[J]. Acta Chimica Sinica, 2012, 0(05): 674-678 .

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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

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