title: Antiviral activity of platinum (II) and palladium (II) complexes of pyridine-2-carbaldehyde thiosemicarbazone.
abstract: A heterocyclic compound, pyridine-2-carbaldehyde thiosemicarbazone (HFoTsc), and its six metal coordinated bound complexes, three with platinum (II) and three with palladium (II), were studied for their activity against herpes simplex virus 1 (HSV-1) infection in cultured cells. According to their cytotoxicity the compounds were divided into two groups. Group I (cytotoxic compounds) included all three palladium complexes and [Pt(HFoTsc)2] Cl2, with maximum non-toxic concentration (MNC) of 1-10 micromol/l and a 50% cytotoxic concentration (CC50) of 20-100 micromol/l. Group 2 (low cytotoxic compounds) with MNC of 100 micromol/l and CC50 of 548-5820 micromol/l included compounds in the following order: [Pt(HFoTsc)2] Cl2<HFoTsc<[PtC] FoTsc)]. The 50% inhibitory concentration (IC50) and a selectivity index (SI) values determined during 24 hrs and 48 hrs of action were indicative of antiviral activity. IC50 and SI values of HFoTsc increased in parallel with the duration of action in HSV-1-infected cells. All three platinum complexes as well as [Pd(HFoTsc)2]Cl2 and [Pd(FoTsc)2] inhibited HSV- I infection following a structure-activity relationship but only [Pt(HFoTsc)2]Cl2 expressed a significant selectivity comparable to that of HFoTsc. However, [PdCl(FoTsc)] acting 48 hrs gave a higher infectious HSV-1 titer (170%) compared to control (100%, no compound).
authors.affiliation: Laboratory of Virology, Faculty of Biology, Sofia University, Bulgaria. t_varadinova@yahoo.com
authors.forename: T
authors.initials: T
authors.lastname: Varadinova
authors.forename: D
authors.initials: D
authors.lastname: Kovala-Demertzi
authors.forename: M
authors.initials: M
authors.lastname: Rupelieva
authors.forename: M
authors.initials: M
authors.lastname: Demertzis
authors.forename: P
authors.initials: P
authors.lastname: Genova
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000494:pharmacology*; D002417:Cattle; D002460:Cell Line; D003588:Cytopathogenic Effect, Viral / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D018259:Herpesvirus 1, Human / Q000187:drug effects* / Q000254:growth & development; D020128:Inhibitory Concentration 50; D009942:Organometallic Compounds / Q000494:pharmacology*; D009944:Organoplatinum Compounds / Q000494:pharmacology*; D010165:Palladium / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013882:Thiosemicarbazones / Q000494:pharmacology*; D013997:Time Factors
chemical_list: D000998:Antiviral Agents; D009942:Organometallic Compounds; D009944:Organoplatinum Compounds; D013882:Thiosemicarbazones; C013996:2-formylpyridine thiosemicarbazone; D010165:Palladium