10-(2-Benzoxazolcarbonyl)-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid
| Autor: | Kevin Capps, Michael P. Hedrick, Stephen J. Benkovic, Ali Tavassoli, Dale L. Boger, Ian A. Wilson, Yan Zhang, Joel Desharnais, Thomas H. Marsilje |
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| Rok vydání: | 2003 |
| Předmět: |
Phosphoribosylglycinamide formyltransferase
biology Phosphoribosylaminoimidazolecarboxamide formyltransferase Stereochemistry Organic Chemistry Clinical Biochemistry Pharmaceutical Science Biochemistry Aminoimidazole Carboxamide Chemical synthesis chemistry.chemical_compound chemistry Enzyme inhibitor Lometrexol Drug Discovery biology.protein Molecular Medicine Tetrahydrofolic acid Purine metabolism Molecular Biology |
| Zdroj: | Bioorganic & Medicinal Chemistry. 11:4503-4509 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/s0968-0896(03)00457-7 |
| Popis: | 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). |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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