{"@context":{"@vocab":"https://cir.nii.ac.jp/schema/1.0/","rdfs":"http://www.w3.org/2000/01/rdf-schema#","dc":"http://purl.org/dc/elements/1.1/","dcterms":"http://purl.org/dc/terms/","foaf":"http://xmlns.com/foaf/0.1/","prism":"http://prismstandard.org/namespaces/basic/2.0/","cinii":"http://ci.nii.ac.jp/ns/1.0/","datacite":"https://schema.datacite.org/meta/kernel-4/","ndl":"http://ndl.go.jp/dcndl/terms/","jpcoar":"https://github.com/JPCOAR/schema/blob/master/2.0/"},"@id":"https://cir.nii.ac.jp/crid/1362825893557533824.json","@type":"Article","productIdentifier":[{"identifier":{"@type":"DOI","@value":"10.1177/095632029901000404"}},{"identifier":{"@type":"URI","@value":"https://journals.sagepub.com/doi/pdf/10.1177/095632029901000404"}},{"identifier":{"@type":"PMID","@value":"10480738"}}],"dc:title":[{"@value":"Anti-Herpesvirus Activities and Cytotoxicities of 2-Thiopyrimidine Nucleoside Analogues <i>in Vitro</i>"}],"description":[{"type":"abstract","notation":[{"@value":"<jats:p> Twenty 2-thiopyrimidine nucleoside analogues were synthesized and examined for inhibitory activity against herpes simplex virus (HSV) type 1 and 2, varicella-zoster virus (VZV), human cytomegalovirus (HCMV) and thymidine kinase-deficient HSV (HSV-TK) replication in vitro. 2-thiouracil (thymine) arabinoside, 2′-deoxy-2-thiouridine (or 2-thiothymidine) and their 5-halogenated derivatives showed anti-HSV activity in both RPMI8226 (human B-lymphoblastoid cells) and MRC-5 (human embryo lung cells). 2′-deoxy-5-halogenated-2-thiocytidines were also inhibitory against HSV, whereas 2-thiocytosine arabinoside and its derivatives were not inhibitory against HSV replication, except 5-bromo and 5-iodo congeners (TN-31, TN-32). Substitution of the halogen atom at the 5-position of the pyrimidine rings to an atom with a higher molecular weight increased anti-HSV and VZV activities, except for the anti-HSV activity of 2-thiouracil arabinosides. 2′-deoxy-5-methyl-, and 2′-deoxy-5-iodo-2-thiouridines (TN-17, TN-44) showed the most potent anti-HSV activity, and 2′-deoxy-5-chloro- and 2′-deoxy-5-bromo-2-thiocytidines were potent inhibitors of VZV replication. However, none of the compounds inhibited HCMV and HSV-TK<jats:sup>−</jats:sup> replication. TN-31 and TN-32 were shown to inhibited HCMV and HSV-TK<jats:sup>−</jats:sup> as well as HSV and VZV replication. The cytotoxicity of the 2-thiopyrimidine nucleoside analogues was less than that of the 2-oxy-congeners of the compounds (5-iodo-2′-deoxyuridine, 5-iodo-2′-deoxycytidine, thymine arabinoside and cytosine arabinoside). The selectivity index of 2′-deoxy-5-iodo-2-thiouridine (TN-44) was higher than that of 5-iodo-deoxyuridine. TN-17 and TN-44 were not cytotoxic to resting or stimulated human peripheral blood mononuclear cells at 400 μ, although TN-32 was cytotoxic at a concentration of 20 μ. </jats:p>"}]}],"creator":[{"@id":"https://cir.nii.ac.jp/crid/1380850475050111746","@type":"Researcher","foaf:name":[{"@value":"S Shigeta"}],"jpcoar:affiliationName":[{"@value":"Department of Microbiology, School of Medicine, Fukushima Medical University, Fukushima, 960-1295, Japan"}]},{"@id":"https://cir.nii.ac.jp/crid/1382825893557533831","@type":"Researcher","foaf:name":[{"@value":"S Mori"}],"jpcoar:affiliationName":[{"@value":"Department of Microbiology, School of Medicine, Fukushima Medical University, Fukushima, 960-1295, Japan"}]},{"@id":"https://cir.nii.ac.jp/crid/1382825893557533830","@type":"Researcher","foaf:name":[{"@value":"T Kira"}],"jpcoar:affiliationName":[{"@value":"Department of Microbiology, School of Medicine, Fukushima Medical University, Fukushima, 960-1295, Japan"}]},{"@id":"https://cir.nii.ac.jp/crid/1382825893557533953","@type":"Researcher","foaf:name":[{"@value":"K Takahashi"}],"jpcoar:affiliationName":[{"@value":"Department of Microbiology, School of Medicine, Fukushima Medical University, Fukushima, 960-1295, Japan"}]},{"@id":"https://cir.nii.ac.jp/crid/1382825893557533828","@type":"Researcher","foaf:name":[{"@value":"E Kodama"}],"jpcoar:affiliationName":[{"@value":"Department of Microbiology, School of Medicine, Fukushima Medical University, Fukushima, 960-1295, Japan"}]},{"@id":"https://cir.nii.ac.jp/crid/1382825893557533954","@type":"Researcher","foaf:name":[{"@value":"K Konno"}],"jpcoar:affiliationName":[{"@value":"Department of Microbiology, School of Medicine, Fukushima Medical University, Fukushima, 960-1295, Japan"}]},{"@id":"https://cir.nii.ac.jp/crid/1382825893557533827","@type":"Researcher","foaf:name":[{"@value":"T Nagata"}],"jpcoar:affiliationName":[{"@value":"Tsukuba Research Laboratory, Toagosei, Tsukuba, 300-2611, Japan"}]},{"@id":"https://cir.nii.ac.jp/crid/1382825893557533829","@type":"Researcher","foaf:name":[{"@value":"H Kato"}],"jpcoar:affiliationName":[{"@value":"Tsukuba Research Laboratory, Toagosei, Tsukuba, 300-2611, Japan"}]},{"@id":"https://cir.nii.ac.jp/crid/1382825893557533824","@type":"Researcher","foaf:name":[{"@value":"T Wakayama"}],"jpcoar:affiliationName":[{"@value":"Tsukuba Research Laboratory, Toagosei, Tsukuba, 300-2611, Japan"}]},{"@id":"https://cir.nii.ac.jp/crid/1382825893557533825","@type":"Researcher","foaf:name":[{"@value":"N Koike"}],"jpcoar:affiliationName":[{"@value":"Tsukuba Research Laboratory, Toagosei, Tsukuba, 300-2611, Japan"}]},{"@id":"https://cir.nii.ac.jp/crid/1382825893557533826","@type":"Researcher","foaf:name":[{"@value":"M Saneyoshi"}],"jpcoar:affiliationName":[{"@value":"Department of Biological Sciences, Teikyo University of Science and Technology, Uenohara, Kitaturu-gun, Yamanashi, 409-0133, Japan"}]}],"publication":{"publicationIdentifier":[{"@type":"PISSN","@value":"09563202"},{"@type":"EISSN","@value":"20402066"},{"@type":"PISSN","@value":"https://id.crossref.org/issn/09563202"}],"prism:publicationName":[{"@value":"Antiviral Chemistry and Chemotherapy"}],"dc:publisher":[{"@value":"SAGE Publications"}],"prism:publicationDate":"1999-08","prism:volume":"10","prism:number":"4","prism:startingPage":"195","prism:endingPage":"209"},"reviewed":"false","dcterms:accessRights":"http://purl.org/coar/access_right/c_abf2","dc:rights":["https://journals.sagepub.com/page/policies/text-and-data-mining-license","http://journals.sagepub.com/page/policies/text-and-data-mining-license"],"url":[{"@id":"https://journals.sagepub.com/doi/pdf/10.1177/095632029901000404"}],"createdAt":"2015-03-16","modifiedAt":"2024-09-04","foaf:topic":[{"@id":"https://cir.nii.ac.jp/all?q=Cell%20Survival","dc:title":"Cell Survival"},{"@id":"https://cir.nii.ac.jp/all?q=Spectrum%20Analysis","dc:title":"Spectrum Analysis"},{"@id":"https://cir.nii.ac.jp/all?q=Humans","dc:title":"Humans"},{"@id":"https://cir.nii.ac.jp/all?q=Nucleic%20Acid%20Conformation","dc:title":"Nucleic Acid Conformation"},{"@id":"https://cir.nii.ac.jp/all?q=Pyrimidine%20Nucleosides","dc:title":"Pyrimidine Nucleosides"},{"@id":"https://cir.nii.ac.jp/all?q=Virus%20Replication","dc:title":"Virus Replication"},{"@id":"https://cir.nii.ac.jp/all?q=Antiviral%20Agents","dc:title":"Antiviral Agents"},{"@id":"https://cir.nii.ac.jp/all?q=Herpesviridae","dc:title":"Herpesviridae"},{"@id":"https://cir.nii.ac.jp/all?q=Cell%20Line","dc:title":"Cell Line"}],"relatedProduct":[{"@id":"https://cir.nii.ac.jp/crid/1390001204166633856","@type":"Article","resourceType":"学術雑誌論文(journal article)","relationType":["isReferencedBy"],"jpcoar:relatedTitle":[{"@language":"en","@value":"Synthesis and Antiviral Activities of Some 4,4'-Dihydroxytriphenylmethanes"},{"@value":"Synthesis and Antiviral Activities of Some 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