Ítem
Acceso Abierto

Synthesis, Antifungal and Antitumor Activity of Novel (Z)-5-Hetarylmethylidene-1,3-thiazol-4-ones and (Z)-5-Ethylidene-1,3-thiazol-4-ones

Mostrar el registro sencillo de la publicación
dc.audienceComunidad Rosaristaspa
dc.creatorInsuasty, Alberto
dc.creatorRamírez, Juan David
dc.creatorRaimondi, Marcela
dc.creatorEcheverry, Carlos
dc.creatorQuiroga, Jairo
dc.creatorAbonia, Rodrigo
dc.creatorNogueras, Manuel
dc.creatorCobo, Justo
dc.creatorRodríguez, María Victoria
dc.creatorZacchino, Susana
dc.creatorInsuasty, Braulio
dc.creator.googleInsuasty, Alberto
dc.creator.googleRamírez, Juan
dc.creator.googleRaimondi, Marcela
dc.creator.googleEcheverry, Carlos
dc.creator.googleQuiroga, Jairo
dc.creator.googleAbonia, Rodrigo
dc.creator.googleNogueras, Manuel
dc.creator.googleCobo, Justo
dc.creator.googleRodríguez, María Victoria
dc.creator.googleZacchino, Susana A.
dc.creator.googleInsuasty, Braulio
dc.date.accessioned2014-08-13T16:30:14Z
dc.date.available2014-08-13T16:30:14Z
dc.date.created2013-05
dc.date.issued2013
dc.description.abstractNew hetaryl- and alkylidenerhodanine derivatives 3a-d, 3e, and 4a-d were prepared from heterocyclic aldehydes 1a-d or acetaldehyde 1e. The treatment of several rhodanine derivatives 3a-d and 3e with piperidine or morpholine in THF under reflux, afforded (Z)-5-(hetarylmethylidene)-2-(piperidin-1-yl) thiazol-4(5H)-ones and 2-morpholinothiazol-4(5H)-ones 5a-d, 6a-d, and (Z)-5-ethylidene-2-morpholinothiazol-4(5H)-one (5e), respectively, in good yields. Structures of all compounds were determined by IR, 1D and 2D NMR and mass spectrometry. Several of these compounds were screened by the U.S. National Cancer Institute (NCI) to assess their antitumor activity against 60 different human tumor cell lines. Compound 3c showed high activity against HOP-92 (Non-Small Cell Lung Cancer), which was the most sensitive cell line, with GI(50) = 0.62 mu M and LC50 > 100 mu M from the in vitro assays. In vitro antifungal activity of these compounds was also determined against 10 fungal strains. Compound 3e showed activity against all fungal strains tested, but showed high activity against Saccharomyces cerevisiae (MIC 3.9 mu g/mL).eng
dc.format.mediumRecurso electrónicospa
dc.format.mimetypeapplication/pdf
dc.format.tipoDocumentospa
dc.identifier.issnISSN:1420-3049
dc.identifier.urihttp://repository.urosario.edu.co/handle/10336/8832
dc.language.isoeng
dc.publisherUniversidad del Rosariospa
dc.relation.citationIssueNo. 5
dc.relation.citationTitleMolecules
dc.relation.citationVolumeVol. 18
dc.relation.ispartofISSN: 1420-3049 MOLECULES V. 18 N. 5 May. 2013spa
dc.relation.urihttp://www.mdpi.com/1420-3049/18/5/5482
dc.rights.accesRightsinfo:eu-repo/semantics/openAccess
dc.rights.accesoAbierto (Texto completo)spa
dc.rights.licenciaEL AUTOR, manifiesta que la obra objeto de la presente autorización es original y la realizó sin violar o usurpar derechos de autor de terceros, por lo tanto la obra es de exclusiva autoría y tiene la titularidad sobre la misma.spa
dc.source.instnameinstname:Universidad del Rosariospa
dc.source.reponamereponame:Repositorio Institucional EdocURspa
dc.subject.ddcEnfermedades
dc.subject.decsBacteriasspa
dc.subject.decsPulmones - Neoplasmasspa
dc.subject.decsCáncerspa
dc.subject.keywordANTIBACTERIAL AGENTSeng
dc.subject.keywordACID-DERIVATIVESeng
dc.subject.keywordCHAINSeng
dc.titleSynthesis, Antifungal and Antitumor Activity of Novel (Z)-5-Hetarylmethylidene-1,3-thiazol-4-ones and (Z)-5-Ethylidene-1,3-thiazol-4-onesspa
dc.typearticleeng
dc.type.hasVersioninfo:eu-repo/semantics/acceptedVersion
dc.type.spaArtículospa
Archivos
Bloque original
Mostrando1 - 1 de 1
Miniatura
Nombre:
molecules-18-05482.pdf
Tamaño:
288.92 KB
Formato:
Adobe Portable Document Format
Descripción:
Descargar
Colecciones
Artículos