Acridine derivatives as anti-BVDV agents |
| |
| Authors: | Tonelli Michele Vettoretti Gerolamo Tasso Bruno Novelli Federica Boido Vito Sparatore Fabio Busonera Bernardetta Ouhtit Aicha Farci Pamela Blois Sylvain Giliberti Gabriele La Colla Paolo |
| |
| Affiliation: | a Dipartimento di Scienze Farmaceutiche, Università di Genova, Viale Benedetto XV 3, 16132 Genova, Italy
b Dipartimento di Scienze e Tecnologie Biomediche, Università di Cagliari, Cittadella Universitaria, S.S. 554, Km 4.500, 09042 Monserrato, Cagliari, Italy |
| |
| 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 EC50 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. |
| |
| Keywords: | ACG, acyclovir Ar, aromatic ring ATCC, American type culture collection AZT, 3&prime -azidothymidine BHK, baby hamster kidney BVDV, bovine viral diarrhea virus CC, column chromatography CCDI50, cell culture infectious dose 50% CVB-5, coxsackie virus, type 5 DMEM, Dulbecco&rsquo s modified Eagle medium DMF, dimethylformamide DMSO, dimethylsulfoxide ds-RNA, double-stranded RNA virus EMCV, encephalomyocarditis virus FBS, fetal bovine serum HIV-1, human immunodeficiency virus, type 1 HCV, hepatitis C virus HSV-1, herpes simplex virus, type 1 HTLV-1, human T-cell leukemia virus type 1 MDBK, Madin Darby bovine kidney MEM-E, Minimum Essential Medium Eagle m.o.i., multiplicity of infection MT-4, CD4+ human T-cells containing an integrated HTLV-1 genome MTT, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide PBS, phosphate buffer solution PFU, Plaque Forming Unit RdRp, RNA-dependent RNA-polymerase Reo-1, Reovirus, type 1 RPMI, Roswell Park Memorial Institut (medium) RSV, respiratory syncytial virus Sb-1, poliovirus type 1-Sabin strain SI, selectivity index ssRNA+, single-stranded positive RNA virus ssRNA&minus , single-stranded negative RNA virus Tris/HCl, tris(hydroxymethyl)aminomethane hydrochloride Vero-76, monkey kidney VSV, vesicular stomatitis virus VV, vaccinia virus YFV, yellow fever virus |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ |
|
