Journal of medicinal chemistry

Novel fluorinated antifolates. Enzyme inhibition and cytotoxicity studies on 2'-and 3'-fluoroaminopterin

J Henkin, WL Washtien

Index: Henkin, Jack; Washtien, Wendy L. Journal of Medicinal Chemistry, 1983 , vol. 26, # 8 p. 1193 - 1196

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Citation Number: 8

Abstract

Two novel analogues of aminopterin with a single fluorine substitution in the 2'(compound 8) or in the 3'(compound 9) position of the p-aminobenzoyl group were synthesized and evaluated as inhibitors of dihydrofolate reductase from two bacterial species and from human HeLa cells. The 2'-fluoro compound was bound essentially the same as aminopterin itself, while the 3'-fluoro derivative bound two-to threefold more tightly in all cases. UV ...