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本文合成了一系列8-去氮-5,6,7,8-四氢甲氨蝶呤类似物作为二氢叶酸还原酶抑制剂并进行了活性评估,结果表明对甲氨蝶呤(MTX)的蝶啶环进行结构改造降低了化合物对二氢叶酸还原酶的抑制活性。
In this paper, a series of 8-deaza-5,6,7,8-tetrahydroc Methotrexate analogues were synthesized and evaluated for their activity as dihydrofolate reductase inhibitors. The results showed that methotrexate (MTX) The structural modification of the pteridine ring reduced the inhibitory activity of the compounds on dihydrofolate reductase.