Journal of medicinal chemistry

Irreversible enzyme inhibitors. 197. Water-soluble reversible inhibitors of dihydrofolate reductase with potent antitumor activity derived from 4, 6-diamino-1, 2-dihydro- …

BR Baker, WT Ashton

文献索引：Baker,B.R.; Ashton,W.T. Journal of Medicinal Chemistry, 1973 , vol. 16, p. 209 - 214

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被引用次数: 27

摘要

A series of 39 derivatives of the title compound was prepared with the object of optimizing reversible inhibition of dihydrofolate reductase and cell membrane transport while achieving sufficient water solubility for effective intravenous administration. Four compounds which met all the criteria were selected for antitumor testing in vivo. Of these, three showed excellent activity against Walker 256 ascites, intramuscular Walker 256, and Dunning leukemia ...