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  • Title: 10-(2-benzoxazolcarbonyl)-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid: a potential inhibitor of GAR transformylase and AICAR transformylase.
    Author: Marsilje TH, Hedrick MP, Desharnais J, Capps K, Tavassoli A, Zhang Y, Wilson IA, Benkovic SJ, Boger DL.
    Journal: Bioorg Med Chem; 2003 Oct 01; 11(20):4503-9. PubMed ID: 13129586.
    Abstract:
    The design and synthesis of 10-(2-benzoxazolcarbonyl)-DDACTHF (1) as an inhibitor of glycinamide ribonucleotide transformylase (GAR Tfase) and aminoimidazole carboxamide transformylase (AICAR Tfase) are reported. Ketone 1 and the corresponding alcohol 13 were evaluated for inhibition of GAR Tfase and AICAR Tfase and the former was found to be a potent inhibitor of recombinant human (rh) GAR Tfase (Ki=600 nM).
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