Journal of medicinal chemistry

Irreversible enzyme inhibitors. CLXXVI. Active-site-directed irreversible inhibitors of dihydrofolate reductase derived from 4, 6-diamino-1, 2-dihydro-2, 2-dimethyl-1- …

BR Baker, WT Ashton

Index: Baker,B.R.; Ashton,W.T. Journal of Medicinal Chemistry, 1970 , vol. 13, # 6 p. 1149 - 1154

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Citation Number: 3

Abstract

Sixteen candidate active-&e-directed irreversible inhibitors of dihydrofolate reductase were synthesized and evaluated for inactivation of the enzyme from L1210 mouse leukemia, Walker 256 rat tumor, rat and mouse liver, and in some instances rat spleen, kidney, and intestine. Thirteen of the sixteen compounds were good to excellent irreversible inhibitors of the enzyme from either L1210 or Walker 256 or both. Tissue specificity with crude enzyme ...