Abstract
Total syntheses from pyridine precursors of 5,10-dideazaaminopterin (1) and 5,10-dideaza-5,6,7,8-tetrahydroaminopterin (2) are described. These compounds exhibit significant in vivo activity against L1210 leukemia that is comparable to that observed with methotrexate.
Publication types
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Comparative Study
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Amide Synthases*
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Aminopterin / analogs & derivatives*
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Aminopterin / chemical synthesis
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Aminopterin / pharmacology
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Aminopterin / therapeutic use
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Animals
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Chemical Phenomena
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Chemistry
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Folic Acid / analogs & derivatives
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Folic Acid / chemical synthesis
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Folic Acid Antagonists
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Leukemia / drug therapy*
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Leukemia L1210 / drug therapy
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Ligases / metabolism
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Male
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Methotrexate / therapeutic use
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Tetrahydrofolates / chemical synthesis
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Thymidylate Synthase / antagonists & inhibitors
Substances
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Folic Acid Antagonists
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Tetrahydrofolates
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lometrexol
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5,10-dideazafolic acid
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Folic Acid
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5,10-dideazaaminopterin
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5,10-dideaza-5,6,7,8-tetrahydroaminopterin
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Thymidylate Synthase
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Ligases
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Amide Synthases
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pteroylpolyglutamate synthase
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Aminopterin
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Methotrexate