中文摘要：

通过5-取代苯基异噁唑-3-甲基胺与2-氰基-3,3-二甲硫基丙烯酸取代酯的缩合反应,合成了一系列含5-取代苯基异噁唑环结构的氰基丙烯酸酯类衍生物,并采用核磁共振波谱和元素分析对化合物的结构进行了表征.初步的生物活性测试结果表明,部分化合物显示出较好的除草活性,在1500 g/ha剂量下,化合物7h,7i和7m对芥菜的茎叶处理抑制率分别为90%,40%和100%;化合物7m和7n对繁缕的茎叶处理抑制率分别为100%和80%;化合物7m和7n对小藜的茎叶处理抑制率分别为100%和85%.此外,化合物7b和7c还表现出良好的抗肿瘤活性,其对HepG2细胞的IC50值分别为3.2和10.1μmol/L.

英文摘要：

In order noacrylates bearing to find novel cyanoacrylate derivatives with potent biological activities, fourteen new cya- a 5-arylisoxazole moiety were synthesized by multistep synthetic procedures with two key intermediates 5 and 6. The intermediate 5 was synthesized from methyl 5-arylisoxazolyl-3-carboxylate via re- duction, chlorination, condensation, and hydrazine cleavage. The structures of target compounds 7 were con- firmed by 1H NMR, 13C NMR and elemental analysis. The bioassay data showed that some target compounds exhibited good herbicidal activities at the dosage of 1500 g/ha. In postemergence treatment, compounds 7h, 7i, and 7m had 90%, 40%, and 100% herbicidal activity against Brassica juncea at 1500 g/ha, compounds 7m and 7n showed 100% and 80% herbicidal activity against Stellaria media at 1500 g/ha, compounds 7m and 7n displayed 100% and 85% inhibitory rates against Chenopodium serotinum L. at 1500 g/ha. In addition, some of the title compounds had satisfactory anti-tumor activities. Compounds 7b and 7c showed wonderful in- hibitory activities against HepG2 cells with the IC50values of 3.2 and 10. 1 μmol/L, respectively.