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  • Title: N10-substituted 5,8-dideazafolate inhibitors of glycinamide ribonucleotide transformylase.
    Author: Caperelli CA.
    Journal: J Med Chem; 1987 Jul; 30(7):1254-6. PubMed ID: 3599031.
    Abstract:
    A series of 5,8-dideazafolates bearing ethyl, isopropyl, cyclopropylmethyl, propargyl, 3-cyanopropyl, carboxymethyl, 2-carboxyethyl, phenacyl, 3-fluorobenzyl, and 5-uracilylmethyl substituents at N10 were tested as inhibitors of purified L5178Y glycinamide ribonucleotide transformylase (GAR TFase), which requires 10-formyltetrahydrofolate as cofactor. All of these cofactor analogues exhibited competitive inhibition against N10-formyl-5,8-dideazafolate, with Ki's ranging from 2 to 32 microM.
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