Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 52, Issue 9, Pages 2979-2988Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm801490z
Keywords
-
Categories
Funding
- University of Antwerp
- Research Foundation Flanders (FWO-Vlaanderen)
- Institute of Promotion of Innovation in Science and Technology of Flanders (IWT)
Ask authors/readers for more resources
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 (MRCS cells), inhibition of beta-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. N-1,N-1-Diethyl-N-4-(5-methyl-5H-indolo[2,3-b]quinolin-8-yl)pentane-1,4-diamine 11c showed an IC50 of 0.01 mu M and a selectivity index of 1800.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available