title: Acridine derivatives as anti-BVDV agents.
abstract: Twenty-six 9-aminoacridine derivatives were evaluated in cell-based assays for cytotoxicity and antiviral activity against a panel of 10 RNA and DNA viruses. While seven compounds (9, 10, 14, 19, 21, 22, 24) did not affect any virus and two (6, 11) were moderately active against CVB-5 or Reo-1, 17 compounds exhibited a marked specific activity against BVDV, prototype of pestiviruses which are responsible for severe diseases of livestock. Most anti-BVDV agents showed EC(50) values in the range 0.1-8 μM, thus comparing favorably with the reference drugs ribavirine and NM 108. Some compounds, particularly those bearing a quinolizidinylalkyl side chain, displayed pronounced cytotoxicity. Further studies are warranted in order to achieve still better anti-BVDV agents, and to explore the potential antiproliferative activity of this kind of compounds.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Genova, Viale Benedetto XV 3, 16132 Genova, Italy. michele.tonelli@unige.it
authors.forename: Michele
authors.initials: M
authors.lastname: Tonelli
authors.forename: Gerolamo
authors.initials: G
authors.lastname: Vettoretti
authors.forename: Bruno
authors.initials: B
authors.lastname: Tasso
authors.forename: Federica
authors.initials: F
authors.lastname: Novelli
authors.forename: Vito
authors.initials: V
authors.lastname: Boido
authors.forename: Fabio
authors.initials: F
authors.lastname: Sparatore
authors.forename: Bernardetta
authors.initials: B
authors.lastname: Busonera
authors.forename: Aicha
authors.initials: A
authors.lastname: Ouhtit
authors.forename: Pamela
authors.initials: P
authors.lastname: Farci
authors.forename: Sylvain
authors.initials: S
authors.lastname: Blois
authors.forename: Gabriele
authors.initials: G
authors.lastname: Giliberti
authors.forename: Paolo
authors.initials: P
authors.lastname: La Colla
mesh_terms: D000166:Acridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000609:Aminoacridines / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D004267:DNA Viruses / Q000187:drug effects*; D001908:Diarrhea Viruses, Bovine Viral / Q000187:drug effects*; D004121:Dimethyl Sulfoxide / Q000737:chemistry; D006801:Humans; D016014:Linear Models; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D012328:RNA Viruses / Q000187:drug effects
chemical_list: D000166:Acridines; D000609:Aminoacridines; D000998:Antiviral Agents; C010847:9-amino-6-chloro-2-methoxyacridine; D004121:Dimethyl Sulfoxide