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dc.contributor.authorDe Lange, Christo
dc.contributor.authorSmit, Frans J.
dc.contributor.authorWentzel, Johannes F.
dc.contributor.authorWong, Ho Ning
dc.contributor.authorHaynes, Richard K.
dc.contributor.authorN'Da, David D.
dc.identifier.citationDe Lange, C. et al. 2018. Synthesis, antimalarial activities and cytotoxicities of amino-artemisinin-1,2-disubstituted ferrocene hybrids. Bioorganic and medicinal chemistry letters, 28(19):3161-3163. []en_US
dc.identifier.issn1464-3405 (Online)
dc.description.abstractArtemisinin-ferrocene conjugates incorporating a 1,2-disubstituted ferrocene analogous to that embedded in ferroquine but attached via a piperazine linker to C10 of the artemisinin were prepared from the piperazine artemisinin derivative, and activities were evaluated against asexual blood stages of chloroquine (CQ) sensitive NF54 and CQ resistant K1 and W2 strains of Plasmodium falciparum (Pf). The most active was the morpholino derivative 5 with IC50 of 0.86 nM against Pf K1 and 1.4 nM against Pf W2. The resistance indices were superior to those of current clinical artemisinins. Notably, the compounds were active against Pf NF54 early and late blood stage gametocytes – these exerted >86% inhibition at 1 µM against both stages; they are thus appreciably more active than methylene blue (∼57% inhibition at 1 µM) against late stage gametocytes. The data portends transmission blocking activity. Cytotoxicity was determined against human embryonic kidney cells (Hek293), while human malignant melanoma cells (A375) were used to assess their antitumor activityen_US
dc.subjectHybrid drugen_US
dc.titleSynthesis, antimalarial activities and cytotoxicities of amino-artemisinin-1,2-disubstituted ferrocene hybridsen_US
dc.contributor.researchID20256353 - De Lange, Christo
dc.contributor.researchID22966390 - Haynes, Richard Kingston
dc.contributor.researchID20883072 - N'Da, David Dago
dc.contributor.researchID20926588 - Smit, Frans Johannes
dc.contributor.researchID20134045 - Wentzel, Johannes Frederik
dc.contributor.researchID25904442 - Wong, Ho Ning

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