{"@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/1390282680713480448.json","@type":"Article","productIdentifier":[{"identifier":{"@type":"DOI","@value":"10.5582/ddt.2012.v6.4.198"}},{"identifier":{"@type":"COI","@value":"1:CAS:528:DC%2BC3sXjtVGnsg%3D%3D"}},{"identifier":{"@type":"PMID","@value":"23006990"}},{"identifier":{"@type":"NAID","@value":"130005054750"}},{"identifier":{"@type":"URI","@value":"https://search.jamas.or.jp/link/ui/2013358421"}}],"resourceType":"学術雑誌論文(journal article)","dc:title":[{"@language":"en","@value":"Synthesis and structure-activity relationship study of 2-(substituted benzylidene)-7-(4-fluorophenyl)-5-(furan-2-yl)-2<i>H</i>-thiazolo[3,2-<i>a</i>]pyrimidin-3(7<i>H</i>)-one derivatives as anticancer agents"},{"@value":"Synthesis and structure-activity relationship study of 2-(substituted benzylidene)-7-(4-fluorophenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a]pyrimidin-3(7H)-one derivatives as anticancer agents"}],"dc:language":"en","description":[{"type":"abstract","notation":[{"@language":"en","@value":"The synthesis and structure-activity relationship (SAR) study of a series of 2-(substituted benzylidene)-7-(4-fluorophenyl)-5-(furan-2-yl)-2<i>H</i>-thiazolo[3,2-<i>a</i>]pyrimidin-3(7<i>H</i>)-one (4a-4j) derivatives as anticancer agents are described. This series of thiazolopyrimidines were synthesized by the reaction of 7-(4-fluoro phenyl)-5-(furan-2-yl)-2<i>H</i>-thiazolo[3,2-<i>a</i>] pyrimidin-3(7<i>H</i>)-one (3) with appropriate substituted aldehydes in the presence of anhydrous sodium acetate and glacial acetic acid. Their structures were confirmed by IR, <sup>1</sup>H-NMR, mass, and elemental analyses. These novel thiazolopyrimidine derivatives were screened for their anticancer activity on the U937 human histocytic lymphoma cell line by 3-(4,5-dimethyl thiazole-2-yl)-2,5-diphenyltetrazoliumbromide (MTT) assay. The comparison of anticancer activity of thiazolopyrimidine was performed considering their structures. This study was done using 2-(substituted benzylidene)-7-(4-fluorophenyl)-5-(furan-2-yl)-2<i>H</i>thiazolo[3,2-<i>a</i>]pyrimidin-3(7<i>H</i>)-one (4a-4j) as a basic model, showing that <i>i</i>) presence of a hydrogen donor/acceptor domain [thiazolo[3,2-<i>a</i>]pyrimidin-3(7<i>H</i>)-one] on the thiazolopyrimidine ring;<i> ii</i>) presence of a hydrophobic [(4-fluorophenyl)] aryl ring system on the thiazolopyrimidine ring;<i> iii</i>) presence of an electron donor moiety [5-(furan-2-yl)] on the thiazolopyrimidine ring; <i>iv</i>) <i>ortho</i> and <i>para</i> substitution of the distal aryl ring [2-(substituted benzylidene)] function strongly influenced anticancer activity. Among these compounds (4a-4j) <i>para </i>substituted derivatives 4c, 4e, 4f, 4g, 4h, and 4j showed significant anticancer activity."}],"abstractLicenseFlag":"disallow"}],"creator":[{"@id":"https://cir.nii.ac.jp/crid/1410282680713480451","@type":"Researcher","personIdentifier":[{"@type":"NRID","@value":"9000283909801"}],"foaf:name":[{"@language":"en","@value":"Panneer Selvam Theivendran"}],"jpcoar:affiliationName":[{"@language":"en","@value":"Department of Pharmaceutical Chemistry, PES's Rajaram and TarabaiBandekar College of Pharmacy"}]},{"@id":"https://cir.nii.ac.jp/crid/1410282680713480450","@type":"Researcher","personIdentifier":[{"@type":"NRID","@value":"9000283909802"}],"foaf:name":[{"@language":"en","@value":"Karthick Viswanathen"}],"jpcoar:affiliationName":[{"@language":"en","@value":"Department of Biotechnology, Acharya Nagarjuna University"}]},{"@id":"https://cir.nii.ac.jp/crid/1410282680713480448","@type":"Researcher","personIdentifier":[{"@type":"NRID","@value":"9000283909803"}],"foaf:name":[{"@language":"en","@value":"Vijayaraj Kumar Palanirajan"}],"jpcoar:affiliationName":[{"@language":"en","@value":"School of Pharmacy, UCSI (University College Sadaya International) University"}]},{"@id":"https://cir.nii.ac.jp/crid/1410282680713480449","@type":"Researcher","personIdentifier":[{"@type":"NRID","@value":"9000283909804"}],"foaf:name":[{"@language":"en","@value":"Ashraf Ali Mohamed"}],"jpcoar:affiliationName":[{"@language":"en","@value":"Institute for Research in Molecular Medicine (INFORM), University of Sains Malaysia"}]}],"publication":{"publicationIdentifier":[{"@type":"PISSN","@value":"18817831"},{"@type":"EISSN","@value":"1881784X"}],"prism:publicationName":[{"@language":"en","@value":"Drug Discoveries & Therapeutics"},{"@language":"ja","@value":"Drug Discoveries & Therapeutics"},{"@language":"en","@value":"DD&T"}],"dc:publisher":[{"@language":"en","@value":"International Research and Cooperation Association for Bio & Socio-Sciences Advancement"},{"@language":"ja","@value":"特定非営利活動法人 バイオ＆ソーシャル・サイエンス推進国際研究交流会"}],"prism:publicationDate":"2012","prism:volume":"6","prism:number":"4","prism:startingPage":"198","prism:endingPage":"204"},"reviewed":"false","url":[{"@id":"https://search.jamas.or.jp/link/ui/2013358421"}],"availableAt":"2012","foaf:topic":[{"@id":"https://cir.nii.ac.jp/all?q=Thiazolopyrimidine","dc:title":"Thiazolopyrimidine"},{"@id":"https://cir.nii.ac.jp/all?q=benzylidene%20aryl%20ring","dc:title":"benzylidene aryl ring"},{"@id":"https://cir.nii.ac.jp/all?q=anticancer%20activity","dc:title":"anticancer activity"}],"dataSourceIdentifier":[{"@type":"JALC","@value":"oai:japanlinkcenter.org:1003620265"},{"@type":"CROSSREF","@value":"10.5582/ddt.2012.v6.4.198"},{"@type":"PUBMED","@value":"23006990"},{"@type":"CIA","@value":"130005054750"}]}