title: Synthesis and structure activity relationships of 5-substituted-4'-thio-beta-D-arabinofuranosylcytosines.
abstract: Four 5-substituted (chloro, fluoro, bromo, methyl) 1-(4-thio-beta-D-arabinofuranosyl)cytosines and their alpha anomers were synthesized by a facile route in high yields. All of these nucleosides were evaluated for cytotoxicity against a panel of human tumor cell lines in vitro. Only 5-fluoro-1-(4-thio-beta-D-arabinofuranosyl)cytosine was found to be highly cytotoxic in all the cell lines and was further evaluated in vivo.
authors.affiliation: Southern Research Institute, Birmingham, Alabama 35255-5305, USA.
authors.forename: K N
authors.initials: KN
authors.lastname: Tiwari
authors.forename: A T
authors.initials: AT
authors.lastname: Shortnacy-Fowler
authors.forename: L
authors.initials: L
authors.lastname: Cappellacci
authors.forename: W R
authors.initials: WR
authors.lastname: Waud
authors.forename: W B
authors.initials: WB
authors.lastname: Parker
authors.forename: J A
authors.initials: JA
authors.lastname: Montgomery
authors.forename: J A
authors.initials: JA
authors.lastname: Secrist
mesh_terms: D001087:Arabinonucleosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013329:Structure-Activity Relationship
chemical_list: D001087:Arabinonucleosides; C411255:4'-thio-arabinofuranosylcytosine