title: Conformationally restricted analogues designed for selective inhibition of GAR Tfase versus thymidylate synthase or dihydrofolate reductase.
abstract: 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.
authors.affiliation: Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, CA 92037, USA. boger@scripps.edu
authors.forename: D L
authors.initials: DL
authors.lastname: Boger
authors.forename: M A
authors.initials: MA
authors.lastname: Labroli
authors.forename: T H
authors.initials: TH
authors.lastname: Marsilje
authors.forename: Q
authors.initials: Q
authors.lastname: Jin
authors.forename: M P
authors.initials: MP
authors.lastname: Hedrick
authors.forename: S J
authors.initials: SJ
authors.lastname: Baker
authors.forename: J H
authors.initials: JH
authors.lastname: Shim
authors.forename: S J
authors.initials: SJ
authors.lastname: Benkovic
mesh_terms: D002460:Cell Line; D002470:Cell Survival; D005493:Folic Acid Antagonists / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D019877:Hydroxymethyl and Formyl Transferases / Q000037:antagonists & inhibitors*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D015394:Molecular Structure; D051026:Phosphoribosylglycinamide Formyltransferase; D013762:Tetrahydrofolate Dehydrogenase / Q000187:drug effects*; D013940:Thymidylate Synthase / Q000037:antagonists & inhibitors*
chemical_list: D005493:Folic Acid Antagonists; D013762:Tetrahydrofolate Dehydrogenase; D013940:Thymidylate Synthase; D019877:Hydroxymethyl and Formyl Transferases; D051026:Phosphoribosylglycinamide Formyltransferase