10-(2-benzoxazolcarbonyl)-5, 10-dideaza-acyclic-5, 6, 7, 8-tetrahydrofolic acid: a potential inhibitor of GAR transformylase and AICAR transformylase

TH Marsilje, MP Hedrick, J Desharnais, K Capps…

Index: Marsilje, Thomas H.; Hedrick, Michael P.; Desharnais, Joel; Capps, Kevin; Tavassoli, Ali; Zhang, Yan; Wilson, Ian A.; Benkovic, Stephen J.; Boger, Dale L. Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 20 p. 4503 - 4509

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Citation Number: 5

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).