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 |
| Item ID: | 54172 |
| Date Deposited: | 31 Jul 2008 |
| Last Modified: | 01 Jun 2011 07:05 |
| Contributors: | Marsilje, T.H. (Author) Hedrick, M.P. (Author) Desharnais, J. (Author) Capps, K. (Author) Tavassoli, A. (Author) Zhang, Y. (Author) Wilson, I.A. (Author) Benkovic, S.J. (Author) Boger, D.L. (Author) |
| Date: | October 2003 |
| Status: | Published |
| URI: | http://eprints.soton.ac.uk/id/eprint/54172 |
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