Abstract
2 min readAbstract 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‐C 5 H 5 ) 2 MCl 2 , Where MTi, V, Mo, Zr and Hf, and (η‐C 5 H 5 ) 2 Tibis(hydrogen maleinate), whereas the metallocenium complexes include the three ferrocenium salts, (η‐C 5 H 5 ) 2 Fe + X − , where X − = trichloroacetate, tetrachloroferrate(III) and picrate, and three recently discovered antitumor titanocenium complexes, i.e. [(η‐C 5 H 5 ) 2 Ti(CH 3 CN)Cl + ] [FeCl ], [(η‐C 5 H 5 ) 2 Ti(2,2′‐bipyridyl) 2+ ][CF 3 SO ] 2 , and [(η‐C 5 H 5 ) 2 Ti( 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‐C 5 H 5 ) 2 Ti(bipy) ] [CF 3 SO ] 2 was active towards the DNA viruses at a concentration that was ten times lower than the cytotoxicity threshold. (η‐C 5 H 5 ) 2 VCL 2 was weakly inhibitory towards HIV reverse transcriptase. All species were ineffective in inhibiting HIV‐induced cytopathogenicity in human T‐lymphocyte MT4 cells.
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