Title
Synthesis and antiplasmodial activity of aminoalkylamino-substituted neocryptolepine derivatives Synthesis and antiplasmodial activity of aminoalkylamino-substituted neocryptolepine derivatives
Author
Faculty/Department
Faculty of Sciences. Chemistry
Faculty of Pharmaceutical, Biomedical and Veterinary Sciences. Pharmacy
Publication type
article
Publication
Washington, D.C. ,
Subject
Pharmacology. Therapy
Source (journal)
Journal of medicinal chemistry. - Washington, D.C., 1963, currens
Volume/pages
52(2009) :9 , p. 2979-2988
ISSN
0022-2623
ISI
000265911800036
Carrier
E
Target language
English (eng)
Full text (Publishers DOI)
Affiliation
University of Antwerp
Abstract
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.
E-info
https://repository.uantwerpen.be/docman/iruaauth/d8a03b/8283146.pdf
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Handle