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Citation: LIU Haibin, LV Ping, PAN Ningning, WANG Wenzhong, WANG Qiang. Synthesis and in vitro Antitumor Activity of 6-Chloro-4-piperazinquinazolinethiosemicarbazone Derivatives[J]. Chinese Journal of Applied Chemistry, ;2012, 29(9): 1000-1005. doi: 10.3724/SP.J.1095.2012.00481 shu

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

1.
School of Biomedicine & Chemical Engineering, Liaoning Institute of Science and Technology, Benxi 117004, China

Corresponding author: LIU Haibin,
Received Date: 1 November 2011
Available Online: 12 March 2012
Fund Project: 辽宁省教育厅科研项目(L2010204) (L2010204)辽宁省高等学校优秀人才支持计划资助(LJQ2011130) (LJQ2011130)辽宁科技学院博士启动金项目(0906B1) (0906B1)

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.
- chloropiperazinquinazoline N-thiosemicarbazone substituted derivatives,
- antitumor activity,
- MTT assay,
- synthesis
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