2，4－二氨基－5－甲基－6－（取代苯胺基）甲基－吡啶〔2，3－4〕并嘧啶类化合物的合成及其定量构效关系

Synthesis of the Compounds 2,4-Diamino-5-Methyl-6-(Substituded Anilino)Methyl-Pyrido(2,3-d) Pyrimidines and Study on the Quantitative Structure-Activity Relationships of the Inhibitory Activity to L_1210 Cell Line

参照ＪＲＰｉｐｅｒ的方法合成了１６个２，４－二氨基－５－甲基－６－（取代苯胺基）甲基－吡啶（２，３－ｄ）并嘧啶类化合物（Ⅲ），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，初步结果为：ｌｏｇ１／Ｃ＝－１．７５（±０．６２）π２＋２．４４（±０．６１）π５，６－１．５７（±０．５０）Σσ＋６．９４（±０．２２）ｎ＝１５，ｒ＝０．９５２，ｓ＝０．２５６还需扩大（Ⅲ）的取代基疏水性参数的变化幅度以进一步研究其构效关系。

By reference to the method of R.J.Piper,sixteen 2,4-diamino-5-methyl-6-(substituted anilino) methyl-pyrido (2,3-d)pyrimidines(Ⅱ)have been synthesized.Their quantitative structure-activity relationships of the inhibitory activity to L1210 cell line have been studied by the Hansch approachThe preliminary result is:log1/C=-175(±062)π2+2.44(±061)π5,6-1.57(±0.50)Σσ+6.94(±0.22)n=15,r=0.952,s=0.256The variation range of the hydrophobic constant of the substituents on the benzene ring of (Ⅱ)has to be enlarged during futher QSAR studies.