Synthesis and Structure-Antitumor Activity of 4,6-Diamino-1,2-Dihydro-2 ,2-Dimethyl-1-(Substituted-Naphthyl- 2)-1,3,5-Triazines

作     者：Li Renli, Sun Guogang and Dai Huacheng (Department of Medicinal Chemistry, Beijing Medical University, Beijing)Yin Jianlin (Institute of Haematology, Chinese Academy of Medical Sciences, Tianjin) 

出 版 物：《Chemical Research in Chinese Universities》 (高等学校化学研究（英文版）)

年 卷 期：1991年第7卷第3期

页      面：197-200页

核心收录：

学科分类：07[理学] 0703[理学-化学] 

基　　金：Supported by the National Natural Science Foundation of China 

主　　题：1-Substituted naphthyl-dihydro-s-triazine Dihydrofolate reductase inhibitor,Quantitative structure-activity relationships(QSAR) 

摘      要：Introduction 4,6-Diamino-1,2-dihydro-2,2-dimethyl-1-substituted-1,3,5-triazines (Ⅰ) are dihydrofolate reductase(DHFR) inhibitors, hence they possess the inhibition to the growth of bacteria and cancer cells. Baker’s antifolate (Ⅱ) has shown promise as an antitumor agertt in clinical trials. The study of the structure-activity relationships of I shows that the inhibition to vertebrate DHFR is significantly influenced by the hydrophobicity of 1-substituent, i.e., the stronger the hydrophobicity of the 1-substituent, the more potent the inhibition of the compound to vertebrate DHFR.