title: Identification of a novel family of nucleosides that specifically inhibit HIV-1 reverse transcriptase.
abstract: N-3-Benzyloxycarbonylmethyl- and N-3-carboxymethyl-TBDMS-substituted nucleosides were synthesized and evaluated for activity against HIV replication. It was found that the N-3-carboxymethyl-TBDMS-substituted nucleosides were specific inhibitors of HIV-1 replication. They should be considered as members of a novel and original class of NNRTIs.
authors.affiliation: Instituto de Química Médica (C.S.I.C.), Juan de la Cierva 3, 28006-Madrid, Spain.
authors.forename: C
authors.initials: C
authors.lastname: Chamorro
authors.forename: E
authors.initials: E
authors.lastname: Lobatón
authors.forename: M C
authors.initials: MC
authors.lastname: Bonache
authors.forename: E
authors.initials: E
authors.lastname: De Clercq
authors.forename: J
authors.initials: J
authors.lastname: Balzarini
authors.forename: S
authors.initials: S
authors.lastname: Velázquez
authors.forename: A
authors.initials: A
authors.lastname: San-Félix
authors.forename: M J
authors.initials: MJ
authors.lastname: Camarasa
mesh_terms: D004353:Drug Evaluation, Preclinical; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D015497:HIV-1 / Q000187:drug effects; D015498:HIV-2 / Q000187:drug effects; D006801:Humans; D009705:Nucleosides / Q000737:chemistry* / Q000494:pharmacology*; D017646:Organosilicon Compounds / Q000737:chemistry; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured / Q000821:virology
chemical_list: D009705:Nucleosides; D017646:Organosilicon Compounds; D018894:Reverse Transcriptase Inhibitors; C404749:tert-butyldimethylsilyl chloride; D054303:HIV Reverse Transcriptase