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dc.creatorOpsenica, Dejan M.
dc.creatorRadivojević, Jelena
dc.creatorMatić, Ivana Z.
dc.creatorŠtajner, Tijana
dc.creatorKnežević-Usaj, Slavica
dc.creatorĐurković-Đaković, Olgica
dc.creatorŠolaja, Bogdan
dc.date.accessioned2021-04-20T12:43:33Z
dc.date.available2021-04-20T12:43:33Z
dc.date.issued2015
dc.identifier.issn0352-5139
dc.identifier.urihttp://rimi.imi.bg.ac.rs/handle/123456789/639
dc.description.abstractNew cyclohexylidene 1,2,4,5-tetraoxanes with polar guanidine and urea based groups were synthesized and evaluated for their antimalarial activity against chloroquine resistant and susceptible Plasmodium falciparum strains. The derivatives showed moderate, nM range antimalarial activities and low cytotoxicity. The N-phenylurea derivative 24 exhibited the best resistance indices (RIW2 = 0.44, RITM91C235 = 0.80) and was not toxic against human normal peripheral blood mononuclear cells (IC50 gt 200 mu M). Seven derivatives were tested in vitro against four human cancer cell lines and they demonstrated high selectivity toward leukaemia K562 cells. One compound, derivative 21 with a primary amino group, was the first tetraoxane tested in vivo against Toxoplasma gondii as another apicomplexan parasite. Subcutaneous administration at a dose of 10 mg kg(-1) day(-1) for 8 days allowed the survival of 20 % of infected mice, thus demonstrating the high potential of tetraoxanes for the treatment of apicomplexan parasites.en
dc.publisherSrpsko hemijsko društvo, Beograd
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172008/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/175011/RS//
dc.rightsopenAccess
dc.rights.urihttps://creativecommons.org/licenses/by-nc-nd/4.0/
dc.sourceJournal of the Serbian Chemical Society
dc.subjectantimalarialsen
dc.subjectantiparasiticen
dc.subjectperoxidesen
dc.subjectcanceren
dc.subjectcytotoxicityen
dc.titleTetraoxanes as inhibitors of apicomplexan parasites Plasmodium falciparum and Toxoplasma gondii growth and anti-cancer moleculesen
dc.typearticle
dc.rights.licenseBY-NC-ND
dc.citation.epage+
dc.citation.issue11
dc.citation.other80(11): 1339-+
dc.citation.rankM23
dc.citation.spage1339
dc.citation.volume80
dc.identifier.doi10.2298/JSC150430063O
dc.identifier.fulltexthttp://rimi.imi.bg.ac.rs/bitstream/id/488/636.pdf
dc.identifier.scopus2-s2.0-84957567719
dc.identifier.wos000366585800001
dc.type.versionpublishedVersion


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