嘧啶類化合物對二氫葉酸還原酶之抑制活性研究   全文下載

Studies on the Inhibition of Bovine Liver Dihydrofolate Reductase by Pyrimidine Compounds

本研究以一系列6-烷基-2,4二胺基嘧啶化合物1-5以及6-甲胺基-2,4-二胺基嘧啶類化合物6-12作牛肝二氧葉酸還原?之抑制試驗。結果顯示6-烷基-2,4二胺基嘧啶化合物具有良好的抑制活性，其IC50在10-7-10-9之間。其中以化合物5之活性最高，其活性與methotrcxatc相當。6- 甲胺基-2,4-二胺基嘧啶類衍生物對該還原?之抑制效果則很低，其IC50在10-4-10-6M之間。"

A series of 6-alky1-2,4-diaminopyrimidines (compounds 1-5) and 6-methylamino-2,4-diaminopyimidines (compounds 6-12), prepared as nonclassical folate antimetabolites, were subjected to inhibition study on bovine liver dihydrofolate reductase. The 2,4-diaminopyrimidine compounds showed IC50's at 10-7-10-9M, with compound 5 as the most active showing comparable activity to that of methotrexate. The triaminopyrimidine analogues 6-12 were much less active, with IG50's ranged between 10-4-10-6M.