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9-吖啶基甲醛芳亚胺席夫碱分别与氯乙酰氯、苄氧乙酰氯在三乙胺作用下产生的烯酮发生[2+2]环加成反应和巯基乙酸的合环反应,合成了9个1-芳基-3-取代-4-(9-吖啶基)-氮杂环丁-2-酮衍生物L1~L6和2-(9-吖啶基)-3-芳基-1,3-噻唑烷-4-酮衍生物T1~T3,对所合成的化合物进行了体外抗癌活性和白细胞共同抗原活性筛选.结构表明,当样品浓度为10μmol/L时,化合物L4对肿瘤细胞HL-60(Leucocythemia人白血病细胞)生长的抑制率为79.4%.当样品浓度为20μg/mL时,化合物L5,L6和T3对细胞分裂周期磷酸酯酶Cdc25B(Cell division cycle 25B phosphatase)的抑制率分别为80.64%,99.75%和99.34%.当样品浓度为20μmol/mL时,化合物L6和T3对CD45(leukocyte common antigen,LCA白细胞共同抗原)蛋白酪氨酸磷酸酶A的抑制率分别为86.12%和91.03%.在此基础上,初步讨论了该类化合物的构效关系.
Schiff base of 9-acridinyl formaldehyde formaldehyde Schiff base and chloroacetyl chloride, benzyloxyacetyl chloride produced by the action of triethylamine [2 + 2] cycloaddition reaction and mercaptoacetic acid ring-closure reaction, Nine 1-aryl-3-substituted-4- (9-acridinyl) -azetidin-2-one derivatives L1 to L6 and 2- (9-acridinyl) 1,3-thiazolidin-4-one derivatives T1 ~ T3, the anti-cancer activity and leukocyte common antigen activity of the synthesized compounds were screened.The structure showed that when the concentration of the sample was 10μmol / L, the compound L4 The inhibition rate of tumor cells HL-60 (Leucocythemia leukemia cells) was 79.4%. When the concentration of the sample was 20μg / mL, the inhibitory effect of compounds L5, L6 and T3 on cell division cycle 25B phosphatase Were 80.64%, 99.75% and 99.34% respectively.When the sample concentration was 20μmol / mL, the inhibitory rates of compound L6 and T3 on protein tyrosine phosphatase A of CD45 (leukemia common antigen) Which is 86.12% and 91.03% respectively.On this basis, the structure-activity relationship of these compounds is discussed preliminarily.