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取代苯甲醛与4-氨基-5-(3,4,5-三甲氧基苯基)-1,2,4-三唑-3-硫酮(2)缩合生成5-(3,4,5-三甲氧基苯基)-4-取代苯基亚胺基-1,2,4-三唑-3-硫酮(3),再烷基加成化为新型5,6-2H-1,2,4-三唑[3,4-b][1,3,4]噻二嗪衍生物4.化合物结构经1H NMR,13C NMR,IR以及元素分析确认.采用噻唑兰(MTT)比色法进行化合物抑制人体前列腺癌细胞(PC3)体外活性测试,结果表明所合成的化合物具有不同程度的抑制PC3活性,其中化合物4a在10μmol?L-1浓度下对PC3的抑制率为75.9%.
Substituted benzaldehyde condenses with 4-amino-5- (3,4,5-trimethoxyphenyl) -1,2,4-triazole-3-thione (2) Trimethoxyphenyl) -4-substituted phenylimino-1,2,4-triazole-3-thione (3) 2,4-triazolo [3,4-b] [1,3,4] thiadiazine derivatives 4. The structures of the compounds were confirmed by 1H NMR, 13C NMR, IR and elemental analysis. MTT colorimetric Compounds were tested in vitro for inhibiting the activity of PC3 in vitro. The results showed that the synthesized compounds inhibited the activity of PC3 to some extent. The inhibitory rate of compound 4a to PC3 was 75.9% under the concentration of 10μmol? L-1.