2,4-二氨基-5-甲基-6-(取代苯胺基)甲基吡啶[2,3-d]并嘧啶类化合物的合成及定量构效关系  

Synthesis and Quantitative Structure Activity Relationships of Lipophilic Antifolate 2,4 Diamino 5 Methyl 6 (Substituted Anilino) Methyl Pyrido[2,3 d]Pyrimidines

作　　者：夏青[1] 吴军[1] 李仁利[1] 

机构地区：[1]北京医科大学药物化学教研室

出　　处：《中国药物化学杂志》1999年第1期40-45,共6页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金

摘　　要：参照文献方法合成了１８个２，４二氨基５甲基６（取代苯胺基）甲基吡啶［２，３ｄ］并嘧啶化合物（Ⅳ），用Ｈａｎｓｃｈ方法研究了它们对Ｌ１２１０细胞株抑制作用的定量构效关系，其结果表明：苯环对位取代基不利于抑制作用。According to the method reported by J.R Piper eighteen 2,4 diamino 5 methyl 6 (substituted anilino)methyl pyrido[2,3 d]pyrimidines(Ⅰ) were synthesized.Combined with the compounds previously reported their structure activity relationships of the inhibition to L 1210 were studied by using the Hansch approach.The correlation equation indicated that substituents on the paraposition of benzene ring were unfavorable to the inhibitory activity,while increasing the bulk of 5′substituent and the hydrophobicity of meta(3′and 5′ positions) substituents would increase the inhibitory activity of this kind of compound.

关 键 词：二氨基吡啶 并嘧啶 抗癌 定量构效关系 合成 

分 类 号：TQ463.54[化学工程—制药化工]