Mutagenicity of New Lead Compounds to Treat Sickle Cell Disease Symptoms in a Salmonella/Microsome Assay

Página do item simplificado
dc.contributor.authordos Santos, Jean Leandro [UNESP]
dc.contributor.authorVaranda, Eliana Aparecida [UNESP]
dc.contributor.authorLima, Lidia Moreira
dc.contributor.authorChin, Chung Man [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionUniversidade Federal do Rio de Janeiro (UFRJ)
dc.date.accessioned2014-05-20T13:24:20Z
dc.date.available2014-05-20T13:24:20Z
dc.date.issued2010-02-01
dc.description.abstractA series of phthalimide derivatives planned as drugs candidates to treat the symptoms of sickle cell anemia were evaluated in a mutagenicity test using strains of Salmonella typhimurium TA100 and TA102, without and with addition of S9 mixture, with the aim to identify the best structural requirements for a drug candidate without genotoxic activity. The compounds (1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl nitrate (1); (1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl nitrate (2); 3-(1,3-dioxo-1,3-dihydro-2H-iso-indol-2-yl)benzyl nitrate (3); 4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-hydroxy-benzenesulfonamide (4); 4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl) benzyl nitrate (5) and 2-[4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)phenyl]ethyl nitrate (6) presented mutagenic potency ranging between 0-4,803 revertants/mu mol. These results allowed us to propose that a methyl spacer linked to a nitrate ester subunit associated to meta aromatic substitution decreases mutagenicity.en
dc.description.affiliationUNESP, Fac Ciencias Farmaceut, Dept Farmacos & Medicamentos, Lapdesf, BR-14801902 Araraquara, SP, Brazil
dc.description.affiliationUNESP, Fac Ciencias Farmaceut, Dept Ciencias Biol, BR-14801902 Araraquara, SP, Brazil
dc.description.affiliationUFRJ, Fac Farm, LASSBio, Ctr Ciencias Saude, BR-21944190 Rio de Janeiro, Brazil
dc.description.affiliationUnespUNESP, Fac Ciencias Farmaceut, Dept Farmacos & Medicamentos, Lapdesf, BR-14801902 Araraquara, SP, Brazil
dc.description.affiliationUnespUNESP, Fac Ciencias Farmaceut, Dept Ciencias Biol, BR-14801902 Araraquara, SP, Brazil
dc.description.sponsorshipCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipIdFAPESP: 07/56115-0
dc.format.extent779-788
dc.identifierhttp://dx.doi.org/10.3390/ijms11020779
dc.identifier.citationInternational Journal of Molecular Sciences. Basel: Mdpi Ag, v. 11, n. 2, p. 779-788, 2010.
dc.identifier.doi10.3390/ijms11020779
dc.identifier.fileWOS000274973500024.pdf
dc.identifier.issn1661-6596
dc.identifier.lattes7501930236496670
dc.identifier.lattes9734333607975413
dc.identifier.orcid0000-0003-4141-0455
dc.identifier.urihttp://hdl.handle.net/11449/7511
dc.identifier.wosWOS:000274973500024
dc.language.isoeng
dc.publisherMdpi Ag
dc.relation.ispartofInternational Journal of Molecular Sciences
dc.rights.accessRightsAcesso aberto
dc.sourceWeb of Science
dc.subjectAMES testen
dc.subjectmutagenicityen
dc.subjectsickle cellen
dc.subjectphthalimide derivativesen
dc.titleMutagenicity of New Lead Compounds to Treat Sickle Cell Disease Symptoms in a Salmonella/Microsome Assayen
dc.typeArtigo
dcterms.licensehttp://www.mdpi.com/about/openaccess
dcterms.rightsHolderMdpi Ag
unesp.author.lattes7501930236496670
unesp.author.lattes9734333607975413[4]
unesp.author.orcid0000-0003-4141-0455[4]
unesp.author.orcid0000-0002-2460-2829[1]
unesp.campusUniversidade Estadual Paulista (Unesp), Faculdade de Ciências Farmacêuticas, Araraquarapt

Arquivos

Pacote Original
Agora exibindo 1 - 1 de 1
Imagem de Miniatura
Nome:
WOS000274973500024.pdf
Tamanho:
190.83 KB
Formato:
Adobe Portable Document Format
Baixar
Licença do Pacote
Agora exibindo 1 - 2 de 2
Nenhuma Miniatura disponível
Nome:
license.txt
Tamanho:
1.71 KB
Formato:
Item-specific license agreed upon to submission
Descrição:
Nenhuma Miniatura disponível
Nome:
license.txt
Tamanho:
1.71 KB
Formato:
Item-specific license agreed upon to submission
Descrição:

Coleções

Artigos - Fármacos e Medicamentos - FCFAR
Artigos - Ciências Biológicas - FCFAR