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Squaric acid/4-aminoquinoline conjugates: novel potent antiplasmodial agents

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dc.contributor.authorRibeiro, Carlos J. A.
dc.contributor.authorKumar, S. P.
dc.contributor.authorGut, Jiri
dc.contributor.authorGonçalves, Lidia M.
dc.contributor.authorRosenthal, Philip J.
dc.contributor.authorMoreira, Rui
dc.contributor.authorSantos, Maria M. M.
dc.date.accessioned2015-04-13T15:57:33Z
dc.date.available2015-04-13T15:57:33Z
dc.date.issued2013
dc.description.abstractWe report the synthesis and structure–activity relationship (SAR) analysis of a series of hybrid compounds containing a squaric moiety conjugated with heterocyclic moieties from well-known antimalarials. This novel series of compounds presents improved antiplasmodial activity compared with the squaric derivatives described in our previous work. Three compounds, 8b (IC50 = 99 nM), 8c (IC50 = 95 nM), and 8d (IC50 = 105 nM) had greater in vitro potency than chloroquine 1 (IC50 = 140 nM) against chloroquine resistant Plasmodium falciparum. In addition, they were noncytotoxic against NIH 3T3 and Hek 293T cells.por
dc.description.sponsorshipThis work was supported by Fundação para a Ciência e a Tecnologia (Portugal) through postdoctoral fellowship to S.P.K. (SFRH/BPD/44481/2008), doctoral fellowship to C.J.A.R. (SFRH/BD/69258/2010) and grant PEst-OE/SAU/UI4013/2011. PJR is a Distinguished Clinical Scientist of the Doris Duke Charitable Foundation.por
dc.identifier.citationEuropean Journal of Medicinal Chemistry 69 (2013) 365-372por
dc.identifier.doihttp://dx.doi.org/10.1016/j.ejmech.2013.08.037
dc.identifier.urihttp://hdl.handle.net/10451/17885
dc.language.isoengpor
dc.peerreviewedyespor
dc.publisherElsevierpor
dc.relationDESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF POTENTIAL CASPASE INHIBITORS USING AS SCAFFOLD QUINONE DERIVATIVES
dc.relationDESIGN AND SYNTHESIS OF SMALL MOLECULE MODULATORS OF P53
dc.relationStrategic Project - UI 4013 - 2011-2012
dc.relation.publisherversionhttp://www.sciencedirect.com/science/article/pii/S0223523413005540por
dc.subjectSquaramidepor
dc.subject4-Aminoquinolinepor
dc.subjectMalariapor
dc.subjectHybridpor
dc.subjectAntiplasmodial activitypor
dc.titleSquaric acid/4-aminoquinoline conjugates: novel potent antiplasmodial agentspor
dc.typejournal article
dspace.entity.typePublication
oaire.awardNumberSFRH/BPD/44481/2008
oaire.awardNumberSFRH/BD/69258/2010
oaire.awardNumberPEst-OE/SAU/UI4013/2011
oaire.awardTitleDESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF POTENTIAL CASPASE INHIBITORS USING AS SCAFFOLD QUINONE DERIVATIVES
oaire.awardTitleDESIGN AND SYNTHESIS OF SMALL MOLECULE MODULATORS OF P53
oaire.awardTitleStrategic Project - UI 4013 - 2011-2012
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/PIDDAC/SFRH%2FBPD%2F44481%2F2008/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/OE/SFRH%2FBD%2F69258%2F2010/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/PEst-OE%2FSAU%2FUI4013%2F2011/PT
oaire.citation.endPage372por
oaire.citation.startPage365por
oaire.citation.titleEuropean Journal of Medicinal Chemistrypor
oaire.citation.volume69por
oaire.fundingStreamPIDDAC
oaire.fundingStreamOE
oaire.fundingStream6817 - DCRRNI ID
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.rightsrestrictedAccesspor
rcaap.typearticlepor
relation.isProjectOfPublication8d05748e-86cd-4825-89a0-2098d13cfb29
relation.isProjectOfPublicationcdcac6bd-b59b-4806-bc18-0d38a2b3f423
relation.isProjectOfPublicationafe1e2c4-bb23-4b69-bb0d-dc960c217226
relation.isProjectOfPublication.latestForDiscoveryafe1e2c4-bb23-4b69-bb0d-dc960c217226

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