含羧酸侧链蒽醛缩氨基均三唑席夫碱衍生物的合成及抗肿瘤活性  

Synthesis and antitumor activity of anthracene-9-carbaldehyde amino-s-triazole Schiff-bases with side-chain of S-acetic acid

作　　者：胡国强[1] 董秀丽 谢松强[1] 黄文龙[3] 

机构地区：[1]河南大学药物研究所,河南开封475001 [2]河南确山县人民医院,河南确山463200 [3]中国药科大学新药中心,江苏南京210009

出　　处：《药学学报》2008年第1期50-53,共4页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(30070861);河南大学重点科研基金资助项目(04ZDZR009).

摘　　要：为发现可用于抗肿瘤活性研究的新结构杂环胺席夫碱先导化合物,本文用氨基均三唑硫代乙酸(2)与9-蒽醛缩合得4-(9-蒽亚甲氨基)-5-苯基-均-三唑-3-硫乙酸席夫碱目标化物(3a^j)。用MTT方法评价了新化合物体外抗肿瘤活性。结果表明,目标化合物对CHO、HL60和L1210三种癌细胞株均有不同程度的细胞毒活性,具有进一步研究的价值。To find out a novel lead compound from heterocyclic amine Schiff bases for developing new antitumor agents, each of （4-amino-5-substituted-s-triazol-3-yhhio）-acetic acids 2a -j was condensed with anthracene-9-carbaldehyde to obtain Schiff-bases of [ 4- （ anthracen-9-yl methylene） amino ] -5-substituteds-triazol-3-ylsulfanyl]-acetic acids 3a -j. The structures of new compounds synthesized Were characterized by elemental analysis and spectral data, and in vitro antitumor activity was also evaluated against CHO, HL60 and L1210 cell lines by MTT assay.

关 键 词：均三唑 硫乙酸 芳醛 席夫碱 抗肿瘤活性 

分 类 号：R916.2[医药卫生—药学]