title: 5'-phosphonate derivatives of 2',3'-dideoxy-3'-thiacytidine as new anti-HIV prodrugs.
abstract: Two new phosphonate 3TC prodrugs were synthesized and studied in MT-4 cells as inhibitors of HIV replication. Their pharmacokinetic parameters were evaluated following intragastric administration in rabbits and oral administration in dogs. Both compounds were much less toxic than parent 3TC in cell cultures and could generate the active nucleoside in laboratory animals.
authors.affiliation: Engelhardt Institute of Molecular Biology, Moscow, Russia.
authors.forename: Anastasia L
authors.initials: AL
authors.lastname: Khandazhinskaya
authors.forename: Maxim V
authors.initials: MV
authors.lastname: Jasko
authors.forename: Inna L
authors.initials: IL
authors.lastname: Karpenko
authors.forename: Pavel N
authors.initials: PN
authors.lastname: Solyev
authors.forename: Natalia A
authors.initials: NA
authors.lastname: Golubeva
authors.forename: Marina K
authors.initials: MK
authors.lastname: Kukhanova
mesh_terms: D000818:Animals; D019380:Anti-HIV Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D002460:Cell Line; D002851:Chromatography, High Pressure Liquid; D004285:Dogs; D004353:Drug Evaluation, Preclinical; D005260:Female; D015497:HIV-1 / Q000187:drug effects / Q000502:physiology; D006801:Humans; D019259:Lamivudine / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D011355:Prodrugs / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D011817:Rabbits; D014779:Virus Replication / Q000187:drug effects
chemical_list: D019380:Anti-HIV Agents; D011355:Prodrugs; D019259:Lamivudine