卤代二甲氧基查尔酮的合成及体外抗宫颈癌活性研究  

Synthesis of halogenated-dimethoxy-chalcone compounds and its anti cervical cancer activity in vitro

作　　者：廖波儿 杨争[1] 木合布力.阿布力孜 任丙昭 杨旭超[1] LIAO Boer;YANG Zheng;Mourboul Ablise;REN Bingzhao;YANG Xuchao(Department of Medicinal Chemistry,College of Pharmacy,Xinjiang Medical University,Urumqi 830011,China)

机构地区：[1]新疆医科大学药学院药物化学有机教研室,乌鲁木齐830011

出　　处：《新疆医科大学学报》2018年第2期237-240,244,共5页Journal of Xinjiang Medical University

基　　金：国家自然科学基金(81260379)

摘　　要：目的合成3种4-卤代-2′,4′-二甲氧基查尔酮,研究其体外抗宫颈癌活性。方法以4-氟苯甲醛、4-氯苯甲醛、4-溴苯甲醛和2,4-二甲氧基苯乙酮为原料,采用EtOH/KOH法制备3种4-卤代-2′,4′-二甲氧基查尔酮,以HeLa和SiHa细胞建立为体外模型,采用MTT法测定其对人子宫癌细胞增殖的抑制活性。结果按以上方法合成得到4-氟-2′,4′-二甲氧基查尔酮(化合物Ⅰ,产率85.35%),4-氯-2′,4′-二甲氧基查尔酮(化合物Ⅱ,产率78.42%)和4-溴-2′,4′-二甲氧基查尔酮(化合物Ⅲ,产率77.88%)。3个化合物作为试药,当药物浓度在50~100μg/mL时,抑制活性在11.34%~94.17%。其中化合物I对HeLa和SiHa细胞作用48h的抑制率分别达到85.87%、93.58%。结论 3种4-卤代-2′,4′-二甲氧基查尔酮对HeLa和SiHa细胞增殖均有较强的抑制活性,其中氟代查尔酮的活性最强,并具有浓度和时间依赖性特点。ObjectiveTo synthesize three kinds of 4-halo-2′,4′-dimethoxy-chalcone compounds and explore their anti-cervical cancer activity in vitro.MethodsThe synthesis of three kinds of 4-Halo-2′,4′-dimethoxy-chalcone were performed by EtOH/KOH base method within 4-Fluorobenzaldehyde,4-Chlorobenzaldehyde,4-Bromobenzaldehyde and 2′,4′-Dimethoxyacetophenone as raw materials;their in vitro anticancer activity were evaluated by using human cervical cancer cells HeLa and SiHa as the experimental model by MTT.ResultsThe 4-fluoro-2′,4′-dimethoxy-chalcone(CompoundⅠ),4-Chloro-2′,4′-dimethoxy-chalcone(CompoundⅡ)and 4-Bromo-2′,4′-dimethoxy-chalcone(CompoundⅢ)were obtained by above method with a yield of 85.35%,78.42%and 77.88%.Three compounds had different inhibitory effects on the proliferation of HeLa and SiHa cancer cells.When the concentration of the drug was 50-100μg/mL,the inhibitory activity was 11.34%-95.28%,in particular.The compound I has a strong inhibitory effect on HeLa and SiHa cells;the maximal inhibition rate was 85.87%to SiH cells and was 93.58%to HeLa cells at 48 h of incubation.ConclusionThe three kinds of 4-halo-2′,4′-dimethoxy-chalcone have strong inhibitory activity against human cervical cancer HeLa and SiHa cells proliferation.The activity of fluoro-chalcone was significantly higher than that of other two halo-chalcone,and their activity was showed concentration and time dependent characteristics.

关 键 词：4-卤代-2′ 4′-二甲氧基查尔酮 化学合成 人子宫癌SiHa和HeLa细胞 抗癌活性 

分 类 号：R914.5[医药卫生—药物化学]