ISSN:
0268-2605
Keywords:
Metallocenes
;
metallocenium complexes
;
antiviral activity
;
DNA viruses
;
RNA viruses
;
HIV-1
;
Chemistry
;
Organic Chemistry
Source:
Wiley InterScience Backfile Collection 1832-2000
Topics:
Chemistry and Pharmacology
Notes:
Six neutral metallocenes and six metallocenium salts, all of which have demonstrated antiproliferative properties, were evaluated for their in vitro broad-spectrum antiviral properties and cytotoxicities. The metallocenes include the compounds (η-C5H5)2MCl2, Where M=Ti, V, Mo, Zr and Hf, and (η-C5H5)2Tibis(hydrogen maleinate), whereas the metallocenium complexes include the three ferrocenium salts, (η-C5H5)2Fe+X-, where X- = trichloroacetate, tetrachloroferrate(III) and picrate, and three recently discovered antitumor titanocenium complexes, i.e. [(η-C5H5)2Ti(CH3CN)Cl+] [FeCl4-], [(η-C5H5)2Ti(2,2′-bipyridyl)2+][CF3SO3-]2, and [(η-C5H5)2Ti(N-methyl-o-aminothiophenolate+)] [I-]. These 12 species were evaluated against DNA viruses (herpes simplex virus type 1, type 2 and vaccinia virus), and RNA viruses [vesicular stomatitis virus, Coxsackie virus B4, Sindbis virus, Semliki forest virus, parainfluenza virus type 3 and human immunodeficiency virus type 1 (HIV-1), the etiologic agent of AIDS]. In the case of HIV-1, the complexes were evaluated for their ability to inhibit HIV-associated reverse transcriptase activity and HIV-1 induced cytopathogenicity in human T-lymphocyte MT4 cells. Selectivity indexes [ratio of the minimum cytotoxic concentration (does) to the minimum (antiviral) inhibitory concentration (dose)] were determined for all complexes and viruses. In general, the netural metallocenes and the ferrocenium salts were only marginally active towards some specific viruses. However,[(η-C5H5)2Ti(bipy)22+] [CF3SO3-]2 was active towards the DNA viruses at a concentration that was ten times lower than the cytotoxicity threshold. (η-C5H5)2VCL2 was weakly inhibitory towards HIV reverse transcriptase. All species were ineffective in inhibiting HIV-induced cytopathogenicity in human T-lymphocyte MT4 cells.
Additional Material:
4 Tab.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1002/aoc.590030605
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