N-(4-(2-乙酰氨基噻唑-4-基)苯基)-3-甲基苯甲酰胺的合成、晶体结构及抗肿瘤活性研究  

Synthesis,Crystal Structure and Anti-tumor Activity of N-(4-(2-Acetylaminothiazol-4-yl)Phenyl)-3-Methylbenzamide

作　　者：周芳 康佳铭 李伟铭 张志华[1] ZHOU Fang;KANG Jia-ming;LI Wei-ming;ZHANG Zhi-hua(School of Chemical and Environmental Engineering,Liaoning University of Technology,Jinzhou 121001,China)

机构地区：[1]辽宁工业大学化学与环境工程学院,辽宁锦州121001

出　　处：《辽宁工业大学学报（自然科学版）》2021年第3期166-169,共4页Journal of Liaoning University of Technology(Natural Science Edition)

基　　金：辽宁省自然科学基金指导计划项目(2019-ZD-0693);国家级大学生创新创业项目(201910154042)。

摘　　要：以α-溴代苯乙酮、硫脲和乙酸酐为原料,采用微波辐射一锅法合成了N-(4-(2-乙酰氨基噻唑-4-基)苯基)-3-甲基苯甲酰胺(3),其结构经^(1)H NMR,^(13)C NMR表征,用X-ray单晶衍射确定(3)的晶体结构。抗肿瘤活性结果表明,化合物(3)人结肠癌细胞株HT29的细胞增殖抑制效果明显,具有进一步的研究价值。N-(4-(2-Acetylaminothiazol-4-yl)phenyl)-3-methylbenzamide(3)was synthesized with three steps,α-bromoacetophenone,thiourea and acetic anhydride used as a raw material.The structures were characterized by ^(1)HNMR,^(13)CNMR and HRMS.The crystal structure of compound(3)was determined by X-ray single crystal diffraction.Preliminary experiments show that the compound(3)can significantly inhibit the proliferation of HT29 tumour cell.The compound(3)may serve as a useful anticancer lead for further optimization and development.

关 键 词：噻唑衍生物 抗肿瘤活性 晶体结构 

分 类 号：O641[理学—物理化学]