title: Synthesis and properties of modified oligonucleotides.
abstract: Phosphorothioate oligonucleotide analogs conjugated to cholesteryl by a neutral, 6 atom linker are more effective inhibitors of HIV-1 in cell culture than the corresponding analogs conjugated via a phosphorothioate group. The antiviral activity correlates with the hydrophobic character of the oligonucleotide. Some new synthetic methodology is also discussed.
authors.affiliation: Department of Chemistry, Northwestern University, Evanston, IL 60208.
authors.forename: R L
authors.initials: RL
authors.lastname: Letsinger
authors.forename: R A
authors.initials: RA
authors.lastname: Alul
authors.forename: F
authors.initials: F
authors.lastname: Farooqui
authors.forename: S M
authors.initials: SM
authors.lastname: Gryaznov
authors.forename: O
authors.initials: O
authors.lastname: Kinstler
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001483:Base Sequence; D002788:Cholesterol Esters / Q000138:chemical synthesis; D015497:HIV-1 / Q000187:drug effects*; D007202:Indicators and Reagents; D008969:Molecular Sequence Data; D009838:Oligodeoxyribonucleotides / Q000138:chemical synthesis; D009841:Oligonucleotides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000998:Antiviral Agents; D002788:Cholesterol Esters; D007202:Indicators and Reagents; D009838:Oligodeoxyribonucleotides; D009841:Oligonucleotides; C027903:oligo (dT)