PMID- 10882019 OWN - NLM STAT- MEDLINE DCOM- 20001103 LR - 20190831 IS - 0968-0896 (Print) IS - 0968-0896 (Linking) VI - 8 IP - 5 DP - 2000 May TI - Conformationally restricted analogues designed for selective inhibition of GAR Tfase versus thymidylate synthase or dihydrofolate reductase. PG - 1075-86 AB - The synthesis and evaluation of a series of conformationally restricted analogues of 10-formyl-tetrahydrofolate as potential inhibitors of glycinamide ribonucleotide transformylase (GAR Tfase) or aminoimidazole carboxamide transformylase (AICAR Tfase) are reported. 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 - Labroli, M A AU - Labroli MA FAU - Marsilje, T H AU - Marsilje TH FAU - Jin, Q AU - Jin Q FAU - Hedrick, M P AU - Hedrick MP FAU - Baker, S J AU - Baker SJ FAU - Shim, J H AU - Shim JH FAU - Benkovic, S J AU - Benkovic SJ LA - eng GR - CA 63536/CA/NCI NIH HHS/United States PT - Journal Article PT - Research Support, Non-U.S. Gov't PT - Research Support, U.S. Gov't, P.H.S. PL - England TA - Bioorg Med Chem JT - Bioorganic & medicinal chemistry JID - 9413298 RN - 0 (Folic Acid Antagonists) RN - EC 1.5.1.3 (Tetrahydrofolate Dehydrogenase) RN - EC 2.1.1.45 (Thymidylate Synthase) RN - EC 2.1.2.- (Hydroxymethyl and Formyl Transferases) RN - EC 2.1.2.2 (Phosphoribosylglycinamide Formyltransferase) SB - IM MH - Cell Line MH - Cell Survival MH - Folic Acid Antagonists/*chemistry/pharmacology MH - Humans MH - Hydroxymethyl and Formyl Transferases/*antagonists & inhibitors MH - Magnetic Resonance Spectroscopy MH - Mass Spectrometry MH - Molecular Structure MH - Phosphoribosylglycinamide Formyltransferase MH - Tetrahydrofolate Dehydrogenase/*drug effects MH - Thymidylate Synthase/*antagonists & inhibitors EDAT- 2000/07/06 11:00 MHDA- 2001/02/28 10:01 CRDT- 2000/07/06 11:00 PHST- 2000/07/06 11:00 [pubmed] PHST- 2001/02/28 10:01 [medline] PHST- 2000/07/06 11:00 [entrez] AID - S0968-0896(00)00051-1 [pii] AID - 10.1016/s0968-0896(00)00051-1 [doi] PST - ppublish SO - Bioorg Med Chem. 2000 May;8(5):1075-86. doi: 10.1016/s0968-0896(00)00051-1.