噁唑、苯并噁唑及1,3,4-噁二唑硫醚的合成及抗肿瘤活性研究有机化学.pdfVIP

2007 年第 27 卷 有 机 化 学 Vol. 27, 2007 第 11 期, 1432～1437 Chinese Journal of Organic Chemistry No. 11, 1432～1437 ·研究简报· 噁唑、苯并噁唑及 1,3,4-噁二唑硫醚的合成及抗肿瘤活性研究 * 张成仁 王 柳 葛燕丽 巨修练 (武汉工程大学化工与制药学院 湖北省新型反应器与绿色化学工艺重点实验室 武汉 430073) 摘要 设计并以噁唑、苯并噁唑及 1,3,4-噁二唑硫醇与卤代烃反应合成了 14 个硫醚类杂环化合物, 其中 13 个化合物未 1 见文献报道. 目标化合物的结构均通过 H NMR 谱、MS 和元素分析进行了表征. 采用 MTT [3-(4,5-dimethylthiagol-2-yl)- 2,5-diphenyltetrogolium bromide]法对 14 个目标化合物进行了体外抗肿瘤活性测定, 结果表明: 在 10－5 mol/L 浓度下, 10 个化合物对肿瘤细胞具有抑制活性. 关键词 噁唑; 苯并噁唑; 1,3,4-噁二唑; 硫醚; 抗肿瘤活性 Synthesis and Antitumor Activity of Oxazol-2-yl, Benzoxazol-2-yl and 1,3,4-Oxadiazol-2-yl Sulfur Ethers ZHANG, Cheng-Ren WANG, Liu GE,Yan-Li JU, Xiu-Lian* (Hubei Key Laboratory of Novel Chemical Reactor and Green Chemical Technology, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, Wuhan 430073) Abstract 14 heterocylic sulfur ethers were designed and synthesized by the reaction of 2-thiol-oxazoles, 2-thiol-benzoxazoles and 2-thiol-1,3,4-oxadiazoles with alkyl halides, respectively, and those of 13 com- 1 pounds have not been reported. All compounds were characterized by MS, H NMR spectra and elemental analysis. The preliminary antitumor activities were investigated by MTT method and the results show that 10 compounds display a content of antitumor activity at the concentration of 10－5 mol/L. Keywords oxazole; be