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

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

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。

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. Keywords：