卡博特韦-1,2,3-三氮唑结构衍生物的合成及抗宫颈癌活性研究  

Synthesis and Anti-Cervical Cancer Activity of Carbotrizole-1,2,3-Triazole Derivatives

作　　者：杨雷鹏 原梦晴 吴紫源 王斓 毛龙飞 王春光 李瑞芳[1] Yang Leipeng;Yuan Mengqing;Wu Ziyuan;Wang Lan;Mao Longfei;Wang Chunguang;Li Ruifang(Henan University of Science and Technology,Luoyang 471023,China;Henan Wanliu Biotechnology Co.,Ltd.,Luoyang 471032,China)

机构地区：[1]河南科技大学,河南洛阳471023 [2]河南湾流生物科技有限公司,河南洛阳471032

出　　处：《山东化工》2024年第18期20-23,共4页Shandong Chemical Industry

基　　金：河南省高等学校重点科研项目计划(23B310001);河南省高等学校重点科研项目计划(24A350006);河南省国际科技合作项目(242102520016);大学生创新创业训练项目(202310464081)。

摘　　要：宫颈癌是女性中常见的恶性肿瘤,而目前的治疗方法副作用显著,对晚期疾病的治疗效果有限,因此亟需研发更好的宫颈癌治疗方法。本研究采用点击化学反应在卡博特韦结构中分别引入带有2-乙基苯基、3,5-二三氟甲基苯基、2-三氟甲氧基苯基、2,5-二三氟甲基苯基、2,4,6-三甲基苯基的1,2,3-三氮唑基团,获得5个结构衍生物,对化合物进行了^(1)H NMR、^(13)C NMR结构表征。并且,以宫颈癌Hela细胞为研究对象,对结构衍生物抗宫颈癌活性进行筛选,采用MTT法检测化合物处理后的Hela细胞存活率。实验结果表明卡博特韦结构衍生物对宫颈癌Hela细胞均具有良好的抗增殖活性,其中化合物C5活性最优。在10μmol/L浓度下,化合物C5处理后Hela细胞存活率为69.18%±1.08%,说明其具有治疗宫颈癌的潜力。Cervical cancer is a common cancer among women,but current treatment methods have significant side effects and limited efficacy in treating advanced cervical cancer.Therefore,there is an urgent need to develop better treatment methods for cervical cancer.In this study,based on the structure of cabotegravir,1,2,3-triazole with substituted group 2-ethylphenyl,3,5-difluoromethylphenyl,2-trifluoromethoxyphenyl,2,5-difluoromethylphenyl,or 2,4,6-trimethylphenyl was introduced to obtain 5 derivatives by click chemistry.The compounds were characterized using^(1)H NMR and^(13)C NMR spectroscopy.Furthermore,the Hela cervical carcinoma cell line was used as the research object to observe the anti-cervical cancer activity of the derivatives.MTT assay was employed to detect the survival rate of Hela cells after treatment with the derivatives.The results showed that all the derivatives exhibited good anti-proliferative activity against Hela cells.Among them,compound C5 showed the best activity,with a cell survival rate of 69.18%±1.08%at a concentration of 10μmol/L,indicating its potential for the treatment of cervical cancer.

关 键 词：宫颈癌 卡博特韦 1 2 3-三氮唑 点击化学 

分 类 号：TQ460[化学工程—制药化工]