Title
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Synthesis and antiplasmodial activity of aminoalkylamino-substituted neocryptolepine derivatives
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Author
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Abstract
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A series of chloro- and aminoalkylamino-substituted neocryptolepine (5-methyl-5H-indolo[2,3-b]quinoline) derivatives were synthesized and evaluated as antiplasmodial agents. The evaluation also included cytotoxicity (MRC5 cells), inhibition of â-hematin formation, and DNA interactions (DNA−methyl green assay). Introduction of aminoalkylamino chains increased the antiplasmodial activity of the neocryptolepine core substantially. The most efficient compounds showed antiplasmodial activities in the nanomolar range. N1,N1-Diethyl-N4-(5-methyl-5H-indolo[2,3-b]quinolin-8-yl)pentane-1,4-diamine 11c showed an IC50 of 0.01 ìM and a selectivity index of 1800. |
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Language
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English
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Source (journal)
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Journal of medicinal chemistry. - Washington, D.C., 1963, currens
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Publication
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Washington, D.C.
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2009
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ISSN
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0022-2623
[print]
1520-4804
[online]
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DOI
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10.1021/JM801490Z
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Volume/pages
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52
:9
(2009)
, p. 2979-2988
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ISI
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000265911800036
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Full text (Publisher's DOI)
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Full text (publisher's version - intranet only)
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