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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Synthesis, β-haematin inhibition, and in vitro antimalarial testing of isocryptolepine analogues: SAR study of indolo[3,2-c]quinolines with various substituents at C2, C6, and N11
Bioorganic and Medicinal Chemistry, Volume 22, No. 9, Year 2014
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Description
A series of indolo[3,2-c]quinolines were synthesized by modifying the side chains of the ω-aminoalkylamines at the C6 position and introducing substituents at the C2 position, such as F, Cl, Br, Me, MeO and NO2, and a methyl group at the N11 position for an SAR study. The in vitro antiplasmodial activities of the derivative agents against two different strains (CQS: NF54 and CQR: K1) and the cytotoxic activity against normal L6 cells were evaluated. The test results showed that compounds 6k and 6l containing the branched methyl groups of 3-aminopropylamino at C6 with a Cl atom at C2 exhibited a very low cytotoxicity with IC50 values above 4000 nM, high antimalarial activities with IC50 values of about 11 nM for CQS (NF54), IC50 values of about 17 nM for CQR (K1), and RI resistance indices of 1.6. Furthermore, the compounds were tested for β-haematic inhibition, and QSAR revealed an interesting linear correlation between the biological activity of CQS (NF54) and three contributing factors, namely solubility, hydrophilic surface area, and β-haematin inhibition for this series. In vivo testing of 6l showed a reduction in parasitaemia on day 4 with an activity of 38%. © 2014 Elsevier Ltd. All rights reserved.
Authors & Co-Authors
Wang, Ning
Japan, Okayama
Okayama University
Wicht, Kathryn Jean
South Africa, Cape Town
University of Cape Town
Imai, Kento
Japan, Okayama
Okayama University
Wang, Mingqi
Japan, Okayama
Okayama University
Anh Ngoc, Tran
Japan, Okayama
Okayama University
Kiguchi, Ryo
Japan, Okayama
Okayama University
Kaiser, Marcel
Switzerland, Allschwil
Swiss Tropical and Public Health Institute Swiss Tph
Switzerland, Basel
Universitat Basel
Egan, Timothy John
South Africa, Cape Town
University of Cape Town
Inokuchi, Tsutomu
Japan, Okayama
Okayama University
Statistics
Citations: 48
Authors: 9
Affiliations: 4
Identifiers
Doi:
10.1016/j.bmc.2014.03.030
ISSN:
09680896
e-ISSN:
14643391