Synthesis of the antileukemic agents 5,10-dideazaaminopterin and 5,10-dideaza-5,6,7,8-tetrahydroaminopterin.

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Taylor EC, Harrington PJ, Fletcher SR, Beardsley GP, Moran RG

Synthesis of the antileukemic agents 5,10-dideazaaminopterin and 5,10-dideaza-5,6,7,8-tetrahydroaminopterin.

J Med Chem. 1985 Jul;28(7):914-21.

PubMed ID

4009615 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Methotrexate	Dihydrofolate reductase	IC 50 (nM)	1.7	N/A	N/A	Details
Methotrexate	Thymidylate synthase	IC 50 (nM)	190000	N/A	N/A	Details