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Cryptolepine analogues containing basic aminoalkyl side-chains at C-11

2008Artigo científico Apenas metadados
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dc.contributor.authorLavrado, Joao
dc.contributor.authorPaulo, Alexandra
dc.contributor.authorGut, Jiri
dc.contributor.authorRosenthal, Philip J.
dc.contributor.authorMoreira, Rui
dc.date.accessioned2015-12-30T10:18:31Z
dc.date.available2015-12-30T10:18:31Z
dc.date.issued2008
dc.description.abstractA series of cryptolepine derivatives has been synthesized through the incorporation of short basic side-chains in the C-11 position of the 10H-indolo[3,2-b] quinoline scaffold. Their antiplasmodial activity was evaluated in vitro against the chloroquine resistant Plasmodium falciparum W2 strain, showing IC50 values between 22 and 184 nM, while their cytotoxicity was assessed using HUVEC cells, revealing three compounds with a selectivity ratio higher than 10. The most selective of these derivatives, 4d, with a selectivity ratio of 46, was also the least cytotoxic of the series. (c) 2008 Elsevier Ltd. All rights reserved.
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dc.identifier.citationBIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - Vol. 18, n. 4 (FEB 15 2008), p. 1378-1381
dc.identifier.doihttp://dx.doi.org/10.1016/j.bmcl.2008.01.015
dc.identifier.issn0960-894X
dc.identifier.urihttp://hdl.handle.net/10451/21632
dc.language.isoeng
dc.publisherPERGAMON-ELSEVIER SCIENCE LTD
dc.subjectChemistry, Medicinal
dc.subjectChemistry, Organic
dc.titleCryptolepine analogues containing basic aminoalkyl side-chains at C-11
dc.titleSynthesis, antiplasmodial activity, and cytotoxicity
dc.typejournal article
dspace.entity.typePublication
oaire.citation.endPage1381por
oaire.citation.startPage1378por
oaire.citation.titleBIOORGANIC & MEDICINAL CHEMISTRY LETTERSpor
oaire.citation.volumeVol. 18por
rcaap.rightsrestrictedAccess
rcaap.typearticle

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