摘要
为得到新型抗肿瘤化合物,以硫代苯甲酰胺衍生物为原料,合成4个新型2-苯基噻唑衍生物,并利用IR,NMR,ESI-MS确定了化合物结构。采用MTT法检测目标化合物对MDA-MB-231乳腺癌细胞增殖的抑制活性,结果表明在100μmol/L浓度下4个化合物对乳腺癌细胞增殖均具有一定的抑制活性。其中,化合物5-(4-(三氟甲基)苯基)-N-((1-(5-(4-(三氟甲基)苯基)噻唑-2-羰基)哌啶-4-基)甲基)噻唑-2-甲酰胺的活性最好,其IC_(50)为24.63μmol/L,优于阳性对照药物阿贝西利(IC_(50)为45.5μmol/L)。2-苯基噻唑衍生物5-(4-(三氟甲基)苯基)-N-((1-(5-(4-(三氟甲基)苯基)噻唑-2-羰基)哌啶-4-基)甲基)噻唑-2-甲酰胺可以作为抗肿瘤药物研发的先导化合物。
To find novel antitumor agents, four novel 2-phenylthiazoles derivatives were synthesized with thiobenzamide derivatives as the starting material. The structures of the compounds were confirmed by IR, NMR and ESI-MS. The inhibitory activities of the target compounds on the proliferation of MDA-MB-231 breast cancer cells were tested by MTT assay. All four compounds had certain inhibitory activities on breast cancer cell proliferation at the concentration of 100 μmol/L. Among them, compound 5-(4-(trifluoromethyl) phenyl)-N-((1-(5-(4-(trifluoromethyl)phenyl)thiazole-2-carbonyl)piperidin-4-yl)methyl)thiazole-2-formamide had the best activity with the IC_(50)of 24.63 μmol/L, which was better than that of the positive control(Verzenio, IC_(50)=45.5 μmol/L). In conclusion, 2-phenylthiazole derivatives 5-(4-(trifluoromethyl)phenyl)-N-((1-(5-(4-(trifluoromethyl)phenyl)thiazole-2-carbonyl)piperidin-4-yl)methyl)thiazole-2-formamide can be used as a lead compound in the development of antitumor drugs.
作者
钱晶晶
武文龙
吉敬
徐誉芯
邹靖培
刘珊鸣
董常娥
史大华
QIAN Jingjing;WU Wenlong;JI Jing;XU Yuxin;ZOU Jingpei;LIU Shanming;DONG Chang’e;SHI Dahua(School of Pharmacy,Jiangsu Ocean University,Lianyungang 222005,China;Jiangsu Key Laboratory of Marine Pharmaceutical Compound Screening,Jiangsu Ocean University,Lianyungang 222005,China;Jiangsu Key Laboratory of Marine Biological Resources and Environment,Jiangsu Ocean University,Lianyungang 222005,China)
出处
《江苏海洋大学学报（自然科学版）》
CAS
2022年第4期68-73,共6页
Journal of Jiangsu Ocean University:Natural Science Edition
基金
江苏省自然科学基金资助项目(BK20191470)
江苏高校优势学科建设工程项目(PAPD)
江苏省研究生科研与实践创新计划项目(KYCX18_2579)。
关键词
抗肿瘤活性
噻唑衍生物
合成
表征
活性评价
antitumor activity
thiazole derivatives
synthesis
characterization
activity evaluation
