title: 5-Fluorocytosine derivatives as inhibitors of deoxycytidine kinase.
abstract: A series of potent piperidine-linked cytosine derivatives were prepared as inhibitors of deoxycytidine kinase (dCK). Compound 9h was discovered to be a potent inhibitor of dCK and shows a good combination of cellular potency and pharmacokinetic parameters. Compound 9h blocks the incorporation of radiolabeled cytosine into mouse T-cells in vitro, as well as in vivo in mice following a T-cell challenge.
authors.affiliation: Lexicon Pharmaceuticals, Princeton, NJ 08540, United States.
authors.forename: James E
authors.initials: JE
authors.lastname: Tarver
authors.forename: Theodore C
authors.initials: TC
authors.lastname: Jessop
authors.forename: Marianne
authors.initials: M
authors.lastname: Carlsen
authors.forename: David J
authors.initials: DJ
authors.lastname: Augeri
authors.forename: Qinghong
authors.initials: Q
authors.lastname: Fu
authors.forename: Jason P
authors.initials: JP
authors.lastname: Healy
authors.forename: Alexander
authors.initials: A
authors.lastname: Heim-Riether
authors.forename: Amy
authors.initials: A
authors.lastname: Xu
authors.forename: Jerry A
authors.initials: JA
authors.lastname: Taylor
authors.forename: Min
authors.initials: M
authors.lastname: Shen
authors.forename: Philip E
authors.initials: PE
authors.lastname: Keyes
authors.forename: S
authors.initials: S
authors.lastname: David Kimball
authors.forename: Xuan-Chuan
authors.initials: XC
authors.lastname: Yu
authors.forename: Maricar
authors.initials: M
authors.lastname: Miranda
authors.forename: Qingyun
authors.initials: Q
authors.lastname: Liu
authors.forename: Jonathan C
authors.initials: JC
authors.lastname: Swaffield
authors.forename: Amr
authors.initials: A
authors.lastname: Nouraldeen
authors.forename: Alan G E
authors.initials: AG
authors.lastname: Wilson
authors.forename: Rick
authors.initials: R
authors.lastname: Finch
authors.forename: Kanchan
authors.initials: K
authors.lastname: Jhaver
authors.forename: Ann Marie Digeorge
authors.initials: AM
authors.lastname: Foushee
authors.forename: Steve
authors.initials: S
authors.lastname: Anderson
authors.forename: Tamas
authors.initials: T
authors.lastname: Oravecz
authors.forename: Kenneth G
authors.initials: KG
authors.lastname: Carson
mesh_terms: D000818:Animals; D003842:Deoxycytidine Kinase / Q000037:antagonists & inhibitors*; D015195:Drug Design; D005437:Flucytosine / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D047428:Protein Kinase Inhibitors; D005437:Flucytosine; D003842:Deoxycytidine Kinase