2-(l-取代-1H-[1,2,3]-三氮唑-4-甲硫基)-5-甲基苯并噁唑化合物的合成及其抗肿瘤活性研究

Synthesis and Antitumor Activities of 2-(1-Substitute-1H-[1,2,3]-Triazol-4-Methylthio)-5-Methylbenzoxazole

以2-氨基-4-甲基苯酚、二硫化碳和3-溴丙炔为原料,经环化、取代、Click反应合成了8个新的2-(l-取代-1H-[1,2,3]-三氮唑-4-甲硫基)-5-甲基苯并噁唑化合物3(a^h)。其结构均经质谱,氢核磁共振和元素分析所确证。经体外抗肿瘤活性测试表明,在20 uM的浓度下,有4个化合物对CDC25B具有较好的抑制活性,其抑制率高达68.18%,IC50可达13.23 ug/mL。

Eight new 2-(1-benzyl-1H-[1,2,3]-triazol-4-methylthio)-5-methylbenzoxazole 3(a^h) were synthe-sized with 2-amino-4-methylphenol, methanedithione and 3-bromoprop-1-yne as starting material, followed by cyclo reaction, substitute reaction and Click reaction. Their structures have been determined by elemental analysis, IR, MS and 1H NMR data. The bioactive assay for the newly pre-pared compounds manifested that four compounds exhibited good inhibitory activity against CDC25B in 20 uM (IC50 value up to 13.23 ug/mL).