title: Synthesis, in vitro anti-HIV and anti-hepatitis B activities and pharmacokinetic properties of amphiphilic heterodinucleoside phosphates containing ddC and AZT.
abstract: Amphiphilic heterodinucleoside phosphates containing AZT and ddC as antiviral monomer were synthesized according to the hydrogenphosphonate method and evaluated in vitro against HIV. dT-N4-pamddC was the most active (IC50 = 40 microM, EC50 = 80 nM) and least toxic (TI = 524) dimer and it exhibited also strong antiviral effects against eight AZT-resistant HIV strains. The ddC-containing heterodimers additionally inhibited HBV replication by 50-80% at 50 microM in Hep G2 2.2.15 cells.
authors.affiliation: Dept. of Pathology, University Hospital, Zürich, Germany.
authors.forename: R A
authors.initials: RA
authors.lastname: Schwendener
authors.forename: P A
authors.initials: PA
authors.lastname: Peghini
authors.forename: P S
authors.initials: PS
authors.lastname: Ludwing
authors.forename: H
authors.initials: H
authors.lastname: Schott
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002460:Cell Line; D015497:HIV-1 / Q000187:drug effects; D006515:Hepatitis B virus / Q000187:drug effects / Q000502:physiology; D006801:Humans; D008826:Microbial Sensitivity Tests; D014779:Virus Replication / Q000187:drug effects; D016047:Zalcitabine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D015215:Zidovudine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D019380:Anti-HIV Agents; D000998:Antiviral Agents; D015215:Zidovudine; D016047:Zalcitabine