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Synthesis and preliminary biological evaluation of 5‐fluoro‐5,8‐dideazaisoaminopterin
Author(s) -
Tomažič Alenka,
Hynes John B.,
Gale Glen R.,
Freisheim James H.
Publication year - 1990
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570270742
Subject(s) - dihydrofolate reductase , chemistry , methotrexate , folic acid antagonists , pharmacology , antagonist , stereochemistry , biological activity , enzyme inhibitor , enzyme , biochemistry , in vitro , medicine , receptor
The new folate antagonist, 5‐fluoro‐5,8‐dideazaisoaminopterin was synthesized in four steps beginning with 2,4‐diamino‐5‐fluoroquinazoline. It was found to be a potent inhibitor of human dihydrofolate reductase. Against L1210 leukemia in mice, 5‐fluoro‐5,8‐dideazaisoaminopterin was equiactive with methotrexate at approximately one half of the total dose employed.