含酰胺结构的新型2-氨基-4-苯基噻唑类化合物的合成及抗癌和抗菌活性研究（英文）

发布时间：2019-04-03 19:46

【摘要】：基于索拉非尼的结构特征设计、合成了一系列含有酰胺结构的新型2-氨基-4-苯基噻唑类化合物.所合成的化合物结构经1H NMR,13C NMR和HRMS表征,并对目标化合物的抗肿瘤和抗菌活性进行了研究.体外抗肿瘤抑制活性结果表明,部分目标化合物显示出较好的活性,特别是N-[3-(2-乙酰氨基噻唑-4-基)苯基]-3-氟苯甲酰胺(4n)对人类结肠癌细胞(HT29)和人肺上皮细胞(A549)细胞株具有显著的抗肿瘤作用,IC50值分别为6.31和7.98μmol·L-1.进一步的研究表明化合物4n可以影响Raf/MEK/ERK信号通路.此外,体外抗菌活性筛选发现,N-[3-(2-乙酰氨基噻唑-4-基)苯基]-3,4-二氯苯甲酰胺(4h)、N-[3-(2-乙酰氨基噻唑-4-基)苯基]-3-氯苯甲酰胺(4i)和N-[3-(2-乙酰氨基噻唑-4-基)苯基]-2,4-二氯苯甲酰胺(4o)对革兰氏阳性菌、革兰氏阴性菌均具有较好抑制作用.
[Abstract]:A series of novel 2-amino-4-phenyl thiazole compounds containing amides were synthesized based on the structural characteristics of sorafinib. The structure of the synthesized compounds was characterized by 1H NMR,13C NMR and HRMS, and the antitumor and antibacterial activities of the target compounds were studied. The results of antitumor activity in vitro showed that some of the target compounds showed good activity. In particular, N-[3-(2-acetylaminothiazole-4-yl) phenyl]-3-fluorobenzamide (4n) had significant antitumor effects on human colon cancer cells (HT29) and human lung epithelial cells (A549). The IC _ (50) values are 6.31 and 7.98 渭 mol 路L ~ (- 1), respectively. Further studies show that compound 4n can affect Raf/MEK/ERK signaling pathway. In addition, screening in vitro showed that N-[3-(2-acetylaminothiazole-4-yl) phenyl]-3,4-dichlorobenzamide (4h), N- [3-(2-acetylaminothiazole-4-yl) phenyl]-3-chlorobenzamide (4i) and N-[3-(2-acetylaminothiazole-4-yl) phenyl]-2,4-dichlorobenzamide (4o) against gram-positive bacteria, Gram-negative bacteria had better inhibitory effect.
【作者单位】：沈阳药科大学生命科学与生物制药学院;辽宁工业大学化学与环境工程学院;沈阳化工研究院生物与医药研究所;锦州医科大学药学院;
【分类号】：O626.25;TQ460.1

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