引用本文:
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.
doi:
10.3724/SP.J.1095.2012.00481
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
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
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
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。
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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
English
Synthesis and in vitro Antitumor Activity of 6-Chloro-4-piperazinquinazolinethiosemicarbazone Derivatives
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.
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