丹皮酚噻唑类化合物的合成及其细胞毒性评价  

Syntheses and Cytotoxicity Evaluation of Novel Paeonol-Thiazoles Derivatives

作　　者：王妙 黄琳[1] 苏燕[1] 许英红 黄铃月 周小群 李芳耀[1] Wang Miao;Huang Lin;Su Yan;Xu Yinghong;Huang Lingyue;Zhou Xiaoqun;Li Fangyao(College of Pharmacy,Guilin Medical University,Guilin 541004;College of Humanities and Management,Guilin Medical University,Guilin 541004)

机构地区：[1]桂林医学院药学院,桂林541004 [2]桂林医学院人文与管理学院,桂林541004

出　　处：《化学通报》2019年第7期630-635,共6页Chemistry

基　　金：广西自然科学基金项目(2016GXNSFAA380323,2018GXNSFAA281200,2016GXNSFEA380001);国家级大学生创新创业训练计划项目(201710601017);桂林市科学研究与技术开发计划重点项目(20170108-10);广西高校中青年科研基础能力提升项目(2019KY051);广西肿瘤免疫与微环境调控重点实验室开放课题项目(2018KF010)资助

摘　　要：本文以丹皮酚为原料合成了15个新型丹皮酚噻唑衍生物,利用IR、1H NMR、13C NMR和MS对所得化合物的结构进行表征,采用MTT法考察了目标化合物对MGC-803(胃癌细胞)、LOVO(结肠癌细胞)、T-24(膀胱癌细胞)3种细胞的体外抗肿瘤活性。结果表明,部分化合物具有良好的细胞毒活性,其中化合物4b、4e、4f、4h、4l对MGC-803的细胞毒性优于阳性对照药顺铂,尤其是化合物4b对MGC-803、LOVO和T-24三种肿瘤细胞的IC50值分别为11.39±4.46、2.06±1.27和6.03±0.86μg/m L,值得进一步研究。Fifteen novel paeonol thiazole derivatives were synthesized using paeonol as starting material and their structures were confirmed by IR,1 H NMR,13 C NMR and MS.All of them were evaluated for their cytotoxicity against three human cancer cell lines(MGC-803,LOVO and T-24)in vitro by standard MTT assay.The results presented that some of the target compounds exhibit significant cytotoxic activity,such as compounds 4 b,4 e,4 f,4 h,4 l exhibite better antitumor activity than the positive reference cisplatin against MGC-803.In particular,compound 4 b shows the most potent antitumor activities with IC50 values of 11.39±4.46μg/m L,2.06±1.27μg/m L and 6.03±0.86μg/m L against MGC-803,LOVO and T-24 tumor cell lines,respectively.It suggestes that compound4 b might be the candidate for further investigation.

关 键 词：丹皮酚 噻唑 合成 细胞毒性 

分 类 号：TQ460.1[化学工程—制药化工]