3-芳基-6-甲基-1,6-二氢-1,2,4,5-四嗪-1(6H)-甲酰胺类化合物的合成及其抗肿瘤活性  

Synthesis and Antitumor Activity of 3-Aryl-6-methyl-1,6-dihydro-1,2,4,5-tetrazine-1-formamide Derivatives

作　　者：张轩赫 裴天运 桑旭杰 陈宇亮 丁雯佳 杨珍珍[1] 徐峰[1] 马良秀 ZHANG Xuanhe;PEI Tianyun;SANG Xujie;CHEN Yuliang;DING Wenjia;YANG Zhenzhen;XU Feng;MA Liangxiu(Taizhou Vocational&Technical College,Taizhou 318000,China;Changzhou University,Changzhou 213164;Tiantai Yisheng Biochemical Technology Co.,Ltd.,Taizhou 317200,China)

机构地区：[1]台州职业技术学院,浙江台州318000 [2]常州大学,江苏常州213164 [3]天台宜生生化科技有限公司,浙江台州317200

出　　处：《合成化学》2023年第9期681-688,共8页Chinese Journal of Synthetic Chemistry

基　　金：2022年浙江省大学生科技创新活动计划项目(2022R481A002);2021年度浙江省高校国内访问工程师“校企合作项目”(FG2021232)。

摘　　要：随着患癌人数逐年增加,抗肿瘤药越来越受到关注。本文以3-芳基-6-甲基-1,2,4,5-四嗪为起始原料,先与硼氢化钠反应得到3-芳基-6-甲基-1,6-二氢-1,2,4,5-四嗪,再与芳基异氰酸酯反应得到目标化合物。通过元素分析、1H NMR、IR和MS表征确认结构后,进一步开展化合物体外对人宫颈癌细胞Hela、人肺癌细胞株A549、人乳腺癌细胞株MCF-7和人白血病细胞株HL-60的抗肿瘤活性测试。以顺铂为对照,发现此类化合物具有一定的体外抗肿瘤活性,其中化合物3j对HL-60的活性接近顺铂,值得进一步研究。As the number of cancer patients increases year by year,antitumor drugs are receiving increasing attention.Using 3-aryl-6-methyl-1,2,4,5-tetrazine as the starting material,3-aryl-6-methyl-1,6-dihydro-1,2,4,5-tetrazine was first reacted with sodium borohydride to obtain 3-aryl-6-methyl-1,6-dihydro-1,2,4,5-tetrazine,and then reacted with arylisocyanate to obtain the target compound.After confirming these structures by elemental analysis,1H NMR,IR and MS characterization,these compounds were further tested for the antitumor activity of human cervical cancer cell line Hela,human lung cancer cell line A549,human breast cancer cell line MCF-7 and human leukemia cell line HL-60 in vitro,and the activity of compound 3j against HL-60 is close to that of cisplatin,with cisplatin as the control.These compounds were found to have certain antitumor activity in vitro,which is worthy of further study.

关 键 词：四嗪 异氰酸酯 顺铂 抗肿瘤活性 合成 

分 类 号：O626.44[理学—有机化学]