title: Synthesis and anti-HIV-1 activities of new pyrimido[5,4-b]indoles.
abstract: A set of new pyrimido[5,4-b]indole derivatives that are structurally related to some non-nucleside HIV-1 reverse transcriptase inhibitors were synthesized and biologically evaluated for their activity as inhibitors of wild and mutant HIV-1 RT types in an 'in vitro' recombinant HIV-1 RT screening assay, as well as anti-infectives in HLT4lacZ-1IIIB cells. Preliminary structure-activity relationships suggest that activity is promoted by simultaneous substitution in positions 2 and 4, especially when chains of alkyldiamine type are present, and by electron-releasing substituents (methoxy) in positions 7 and 8. The inactivity or the very low activity of title derivatives does not suggest interest in AIDS therapy.
authors.affiliation: Departamento Química Orgànica y Farmacéutica, Universidad de Navarra, Pamplona, Spain.
authors.forename: I
authors.initials: I
authors.lastname: Merino
authors.forename: A
authors.initials: A
authors.lastname: Monge
authors.forename: M
authors.initials: M
authors.lastname: Font
authors.forename: J J
authors.initials: JJ
authors.lastname: Martínez de Irujo
authors.forename: E
authors.initials: E
authors.lastname: Alberdi
authors.forename: E
authors.initials: E
authors.lastname: Santiago
authors.forename: I
authors.initials: I
authors.lastname: Prieto
authors.forename: J J
authors.initials: JJ
authors.lastname: Lasarte
authors.forename: P
authors.initials: P
authors.lastname: Sarobe
authors.forename: F
authors.initials: F
authors.lastname: Borrás
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D019380:Anti-HIV Agents; D007211:Indoles; D018894:Reverse Transcriptase Inhibitors