PMID- 10888335 OWN - NLM STAT- MEDLINE DCOM- 20001107 LR - 20190819 IS - 0960-894X (Print) IS - 0960-894X (Linking) VI - 10 IP - 13 DP - 2000 Jul 3 TI - Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase. PG - 1471-5 AB - The examination results of a novel series of potential inhibitors of glycinamide ribonucleotide transformylase (GAR Tfase) and aminoimidazole carboxamide transformylase (AICAR Tfase) are reported. These agents incorporate an electrophilic fluoronitrophenyl group that can potentially react with an active site nucleophile or the substrate GAR/AICAR amine via nucleophilic aromatic substitution. FAU - Boger, D L AU - Boger DL AD - Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, CA 92037, USA. boger@scripps.edu FAU - Marsilje, T H AU - Marsilje TH FAU - Castro, R A AU - Castro RA FAU - Hedrick, M P AU - Hedrick MP FAU - Jin, Q AU - Jin Q FAU - Baker, S J AU - Baker SJ FAU - Shim, J H AU - Shim JH FAU - Benkovic, S J AU - Benkovic SJ LA - eng PT - Journal Article PL - England TA - Bioorg Med Chem Lett JT - Bioorganic & medicinal chemistry letters JID - 9107377 RN - 0 (Enzyme Inhibitors) RN - 0 (Nitro Compounds) RN - 0 (Purines) RN - 0 (Ribonucleotides) RN - 284SYP0193 (Fluorine) RN - 935E97BOY8 (Folic Acid) RN - EC 2.1.2.- (Hydroxymethyl and Formyl Transferases) RN - EC 2.1.2.2 (Phosphoribosylglycinamide Formyltransferase) SB - IM MH - Animals MH - Biological Assay MH - Combinatorial Chemistry Techniques MH - Drug Design MH - Enzyme Inhibitors/*chemical synthesis/pharmacology MH - Fluorine/chemistry MH - Folic Acid/*analogs & derivatives/pharmacology MH - Hydroxymethyl and Formyl Transferases/*antagonists & inhibitors MH - Molecular Structure MH - Nitro Compounds/*chemical synthesis MH - Phosphoribosylglycinamide Formyltransferase MH - Precursor Cell Lymphoblastic Leukemia-Lymphoma MH - Purines/biosynthesis MH - Ribonucleotides/*metabolism MH - Tumor Cells, Cultured EDAT- 2000/07/11 11:00 MHDA- 2001/02/28 10:01 CRDT- 2000/07/11 11:00 PHST- 2000/07/11 11:00 [pubmed] PHST- 2001/02/28 10:01 [medline] PHST- 2000/07/11 11:00 [entrez] AID - S0960-894X(00)00271-7 [pii] AID - 10.1016/s0960-894x(00)00271-7 [doi] PST - ppublish SO - Bioorg Med Chem Lett. 2000 Jul 3;10(13):1471-5. doi: 10.1016/s0960-894x(00)00271-7.