首页|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

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

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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1H NMR、13C 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 10 μmol/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。
Synthesis and Anti-Cervical Cancer Activity of Carbotrizole-1,2,3-Triazole Derivatives
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 1H NMR and 13C 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 10 μmol/L,indicating its potential for the treatment of cervical cancer.

cervical cancercabotegravir1,2,3-triazoleclick chemistry

杨雷鹏、原梦晴、吴紫源、王斓、毛龙飞、王春光、李瑞芳

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河南科技大学,河南 洛阳 471023

河南湾流生物科技有限公司,河南 洛阳 471032

宫颈癌 卡博特韦 1,2,3-三氮唑 点击化学

河南省高等学校重点科研项目计划河南省高等学校重点科研项目计划河南省国际科技合作项目大学生创新创业训练项目

23B31000124A350006242102520016202310464081

2024

山东化工
山东省化工研究院 山东省化工信息中心

山东化工

影响因子:0.249
ISSN:1008-021X
年,卷(期):2024.53(18)
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