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


Marsilje, T.H., Hedrick, M.P., Desharnais, J., Capps, K., Tavassoli, A., Zhang, Y., Wilson, I.A., Benkovic, S.J. and Boger, D.L. (2003) 10-(2-benzoxazolcarbonyl)-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid: A potential inhibitor of GAR transformylase and AICAR transformylase. Bioorganic & Medicinal Chemistry, 11, (20), 4503-4509. (doi:10.1016/S0968-0896(03)00457-7).

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Description/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).

Item Type: Article
ISSNs: 0968-0896 (print)
Related URLs:
Keywords: 8, functionalized analogs, beta-gar, catalyzed-hydrolysis, crystal-structure, tfase, folate analogs, selective-inhibition, 10-formyl-5,glycinamide ribonucleotide transformylase, amide,10-trideazafolic acid, hydrolase
Subjects: Q Science
Q Science > QD Chemistry
Divisions: University Structure - Pre August 2011 > School of Chemistry
ePrint ID: 54172
Date Deposited: 31 Jul 2008
Last Modified: 27 Mar 2014 18:37
URI: http://eprints.soton.ac.uk/id/eprint/54172

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