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  • Organic Chemistry  (5)
  • RNA viruses  (2)
  • Antiviral agents  (1)
  • 1
    Electronic Resource
    Electronic Resource
    Inhibition of fluorouracil catabolism in cancer patients by the antiviral agent (E)-5-(2-bromovinyl)-2′-deoxyuridine (1994)
    Springer
    Journal of cancer research and clinical oncology 120 (1994), S. 545-549 
    Details
    ISSN: 1432-1335
    Keywords: Fluorouracil catabolism ; Bromovinyl-deoxyuridine ; Antiviral agents ; Dehydrouracil dehydrogenase
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The thymidine analogue (E)-5-(2-bromovinyl)-2′-deoxyuridine (BVdUrd), which is an antiviral agent effective against herpes simplex virus type 1 and varicella zoster virus, has also proved to be a potent inhibitor of dihydrouracil dehydrogenase, the major degrading enzyme of the anticancer drug fluorouracil (FUra). To evaluate the effect of BVdUrd on the pharmacokinetics of FUra in cancer patients, BVdUrd was administered orally at a daily dose of 250 mg (five patients) or 3×250 mg (five patients). FUra was infused at doses of 110–400 mg over 10 min. Blood and urine samples were collected regularly during a period of up to 50 h. BVdUrd was rapidly absorbed, peak plasma levels of 0.6–7.1 μg/ml being achieved after 1–2 h. Following a rapid decline, plasma BVdUrd levels remained higher than 10 ng/ml for up to 2 days after BVdUrd administration. The total body clearance of FUra was approximately 6 l/h andt 1/2 markedly increased to 4–7 h. The mean urinary excretion of FUra was 50%. No differences in FUra kinetics were observed between patients receiving one or three oral doses of BVdUrd. We conclude that the concomitant use and subsequent interaction of FUra and the antiviral agent BVdUrd resulted in an impressive inhibition of FUra breakdown and marked increase of renal clearance. The findings indicate that the simultaneous use of FUra and drugs resembling this antiviral agent in patients may result in unexpected toxicity. Further experience with BVdUrd and new analogues might enable the development of new FUra treatment schedules and treatment designs e.g. combinations with leucovorin.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01221032
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  • 2
    Electronic Resource
    Electronic Resource
    Synthesis and Biological Activities of C (5)-N-Spin-Labeled Uridines and Related DerivativesDedicated to Prof. Dr. Max Viscontini on the occasion of his 70th birthday (1983)
    New York, NY : Wiley-Blackwell
    Helvetica Chimica Acta 66 (1983), S. 534-541 
    Details
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Direct introduction of a N-atom in one step at C (5) of 5-hydroxyuridine (4a) or 5-hydroxy-2′-deoxyuridine (4b) by certain primary amines led to the synthesis of two novel C(5)-N-spin-labeled nucleoside analogs and to several C(5)-N-aryl adducts. Substitution by 4-amino-2,2,6,6-tetramethylpiperidinooxyl (3) at C(5) of 4a or 4b led to the spin-labeled nucleosides 5-[(1-oxyl-2,2,6,6-tetramethyl-4-piperidinyl)amino]uridine and -2′-deoxyuridine (2a and 2b, respectively). The analogous C(5)-substituted aniline adducts 5-anilino uridine (5a) and 5-anilino-2′-deoxyuridine (5b) and the p-toluidine adducts 5-(p-toluidino)uridine (6a) and 5-(p-toluidino)-2-deoxyuridine (6b) were also prepared. In addition, results of the antiviral and antimetabolic activity of some of these analogs are reported.
    Additional Material: 1 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/hlca.19830660214
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  • 3
    Electronic Resource
    Electronic Resource
    Nucleotides. Part. XXXIIPart XXXI: [1].. Synthesis of 2′-5′ Connected oligonucleotides. Prodrugs for antiviral and antitumoral nucleosides (1989)
    New York, NY : Wiley-Blackwell
    Helvetica Chimica Acta 72 (1989), S. 1739-1748 
    Details
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The cytotoxically and antivirally active compounds bvUd (1), flUd (4), acyclovir (7), and Aa (12) have chemically been combined with the appropriately protected (2′-5′)diadenylate 20 by the phosphotriester approach to give the 2′-5′ oligonucleotide trimers 21-24. The deprotection of the various blocking groups by chemical means afforded the 2′-5′ trimers 25-28, which can be regarded as new type of a potential prodrug form delivering nucleotides to the targets inside cells. In an analogous series of reactions, 9-(3′-azido-3′-deoxy-β-D-xylofuranosyl)adenine was coupled with 7 to the 2′-5′ trimer 31. The antiviral screening of the oligonucleotides 25-27 and 31 showed biological activities closely related to the parent nucleosides, possibly indicating their release by enzymatic cleavage of the oligomers.
    Additional Material: 1 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/hlca.19890720811
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  • 4
    Electronic Resource
    Electronic Resource
    Synthesis of 2′-Deoxy-5-(isothiazol-5-yl)uridine and Its Interaction with the HSV-1 Thymidine Kinase (1996)
    New York, NY : Wiley-Blackwell
    Helvetica Chimica Acta 79 (1996), S. 1462-1474 
    Details
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: 2′-Deoxy-5-(isothiazol-5-yl)uridine (12) was synthesized starting from 2′-deoxy-5-iodouridine using a Pd-catalysed cross-coupling reaction with propiolaldehyde diethyl acetal followed by deprotection and ring closure using thiosulfate. 2′-Deoxyuridine 12 has a particular place among the 5-heteroaryl-substituted 2′-deoxyuridines in that it has a high affinity for herpes simplex virus type 1 (HSV-1)-encoded thymidine kinase (TK) without antiviral activity. Biochemical studies revealed that 12 is a substrate for viral TK. We further investigated the interaction of 12 with the HSV-1 thymidine kinase. The conformation of 12 in solution was established by NMR spectroscopy. The most stable conformer 12A has the S-atom of the isothiazole ring placed in the neighbourhood of the C(4)=O group of the pyrimidine moiety. The compound was docked in its most stable conformation in the active site of HSV-1 TK and subjected to energy minimization. This demonstrated that the isothiazole moiety binds in a cavity lined by the side chains of Tyr-132, Arg-163, Ala-167, and Ala-168 and that the C(3) atom of the isothiazole moiety is located in close proximity of the phenolic O-atom of Tyr-132 and the aliphatic part of the Arg-163 side chain.
    Additional Material: 6 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/hlca.19960790519
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  • 5
    Electronic Resource
    Electronic Resource
    Assessment of the in vitro broad-spectrum antiviral activity of some selected antitumor metallocene and metallocenium complexes (1989)
    New York, NY [u.a.] : Wiley-Blackwell
    Applied Organometallic Chemistry 3 (1989), S. 491-497 
    Details
    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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  • 6
    Electronic Resource
    Electronic Resource
    Assessment of the in vitro broad-spectrum antiviral activity of some selected antitumor organotin complexes (1989)
    New York, NY [u.a.] : Wiley-Blackwell
    Applied Organometallic Chemistry 3 (1989), S. 431-436 
    Details
    ISSN: 0268-2605
    Keywords: Organotin complexes ; octahedral ; antitumor ; DNA viruses ; RNA viruses ; HIV ; Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Eleven antitumor-active octahedral organotin complexes of the type R2SnX2L2, where R = methyl, ethyl or phenyl, X = chloride or bromide, and L2 = o-phenantholine ((phen), 2-)2-(pyridyl)-benzimidazole (PBI) or two dimethylsulfoxides (2DMSO), were examined for their broad-spectrum in vitro antiviral activity against a number of DNA and RNA viruses. The DNA viruses included in this study were herpes simplex virus type 1 and type 2, a TK-(thymidine kinase deficient) strain of herpes simplex virus type 1, and vaccinia virus. The RNA viruses were vesicular stomatitis virus, Coxsackie virus type B4, Sindbis virus, Semliki forest virus, parainfluenza virus type 3, and human immunodeficiency virus (HIV). Overall, the complexes showed weak antiviral activity and low selectivity. With the exception of (CH3)2SnBr2·PBI and (C6H5)2SnCl2·2DMSO, all of the complexes were active against one or more of the three strains of herpes simplex viruses. On the other hand, only three complexes, (CH3)2SnBr2·PBI, (CH3)2SnBr2·phen, and (C6H5)5SnBr2·PBI, exhibited marginal activity against some of the RNA viruses. None of the complexes was active against vesicular stomatitis or parainfluenza virus. Similarly, there was no inhibitory activity towards HIV-1-associated reverse transcriptase or HIV-1-induced cytopathogenicity in human T-lymphocyte MT4 cell cultures at subtoxic concentrations.
    Additional Material: 4 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/aoc.590030509
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