New Spiro-acridines: Dna Interaction, Antiproliferative Activity And Inhibition Of Human Dna Topoisomerases

dc.creatorVitalino de Almeida
dc.creatorSinara Monica; Lafayett
dc.creatorElizabeth Almeida; Silva
dc.creatorWillams Leal; Serafim
dc.creatorVanessa de Lima; Menezes
dc.creatorThais Meira; Neves
dc.creatorJorge Luiz; Tasca Gois Ruiz
dc.creatorAna Lucia; de Carvalho
dc.creatorJoao Ernesto; de Moura
dc.creatorRicardo Olimpio; Carneiro Beltrao
dc.creatorEduardo Isidoro; de Carvalho Junior
dc.creatorLuiz Bezerra; Alves de Lima
dc.creatorMaria do Carmo
dc.date2016
dc.datenov
dc.date2017-11-13T13:54:22Z
dc.date2017-11-13T13:54:22Z
dc.date.accessioned2018-03-29T06:07:46Z
dc.date.available2018-03-29T06:07:46Z
dc.identifierInternational Journal Of Biological Macromolecules. Elsevier Science Bv, v. 92, p. 467 - 475, 2016.
dc.identifier0141-8130
dc.identifier1879-0003
dc.identifierWOS:000386402900056
dc.identifier10.1016/j.ijbiomac.2016.07.057
dc.identifierhttp://www-sciencedirect-com.ez88.periodicos.capes.gov.br/science/article/pii/S0141813016308911?via%3Dihub
dc.identifierhttp://repositorio.unicamp.br/jspui/handle/REPOSIP/329382
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1366407
dc.descriptionConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.descriptionCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.descriptionTwo new spiro-acridines were synthesized by introducing cyano-N-acylhydrazone between the acridine and phenyl rings followed by spontaneous cyclization. The final compounds (E)-1'-(benzylideneamino)-5'-oxo-1',5'-dihydro-10H-spiro[acridine-9,2'-pyrrole]-4'-carbonitrile (AMTAC-01) and (E)-1'-((4-methoxybenzylidene)amino)-5'-oxo-1',5'-dihydro-10H-spiro[acridine-9,2'-pyrrole]-4'-carbonitrile (AMTAC-02) were evaluated for their interactions with calf thymus DNA, antiproliferative and human topoisomerase I and II alpha inhibitory activities. Both compounds presented ability to bind DNA. The binding constant determined by UV-vis spectroscopy was found to be 10(4)M(-1). Antiproliferative assay demonstrated that AMTAC-01 and AMTAC-02 were most active against prostate and melanoma tumor cell lines, respectively. The compound did not present Topo I inhibitory activity. However, both derivatives displayed topoisomerase IIa inhibitory activity comparable to amsacrine, and AMTAC-02 was more potent than AMTAC-01 with methoxy substituent group on phenyl ring. This study demonstrates that the new derivatives are promising molecules with topoisomerase II alpha inhibitory and antiproliferative activities. (C) 2016 Elsevier B.V. All rights reserved.
dc.description92
dc.description467
dc.description475
dc.descriptionCNPq (Conselho Nacional de Desenvolvimento Cientifico e Tecnologico, Brazil)
dc.descriptionCAPES (Fundacao Coordenacao de Aperfeicoamento de Pessoal de Ensino Superior, Brazil)
dc.descriptionFACEPE (Fundo de Amparo a Ciencia e Tecnologia de Pernambuco, Brazil) [APQ-0903-4.03/15]
dc.descriptionConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.descriptionCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.languageEnglish
dc.publisherElsevier Science BV
dc.publisherAmsterdam
dc.relationInternational Journal of Biological Macromolecules
dc.rightsfechado
dc.sourceWOS
dc.subjectSpiro-acridine
dc.subjectDna-binding
dc.subjectTopoisomerase
dc.titleNew Spiro-acridines: Dna Interaction, Antiproliferative Activity And Inhibition Of Human Dna Topoisomerases
dc.typeArtículos de revistas


Este ítem pertenece a la siguiente institución