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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Synthesis and in vitro antimalarial testing of neocryptolepines: SAR study for improved activity by introduction and modifications of side chains at C2 and C11 on indolo[2,3-b]quinolines
Journal of Medicinal Chemistry, Volume 56, No. 4, Year 2013
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Description
To obtain a high antimalarial activity with neocryptolepine derivatives, modifying and changing the side chains at the C11 position with varying the substituents of an electron-withdrawing or electron-donating nature at the C2 position for a SAR study were executed. Installation of alkylamino and ω-aminoalkylamino groups at the C11 position of the neocryptolepine core was successful. For further variation, the aminoalkylamino substituents were transformed into the corresponding acyclic or cyclic carbamides or thiocarbamides. These side chain modified neocryptolepine derivatives were tested for antimalarial activity against CQR (K1) and CQS (NF54) of Plasmodium falciparum in vitro and for cytotoxicity toward mammalian L6 cells. Among the tested compounds, the compound 17f showed an IC50 of 2.2 nM for CQS (NF54) and a selectivity index of 1400, and 17i showed an IC50 of 2.2 nM for CQR (K1), a selectivity index of 1243, and a resistance index of 0.5. © 2013 American Chemical Society.
Authors & Co-Authors
Mei, Zhen Wu
Japan, Okayama
Okayama University
Wang, Li
Japan, Okayama
Okayama University
Lu, Wenjie
Japan, Okayama
Okayama University
Pang, Cui Qing
Japan, Okayama
Okayama University
Maeda, Tsukasa
Japan, Okayama
Okayama University
Peng, Wei
Japan, Okayama
Okayama University
Kaiser, Marcel
Switzerland, Allschwil
Swiss Tropical and Public Health Institute Swiss Tph
Switzerland, Basel
Universitat Basel
El-Tantawy El-Sayed, Ibrahim Tantawy
Japan, Okayama
Okayama University
Egypt, Shibin el Kom
Menoufia University
Inokuchi, Tsutomu
Japan, Okayama
Okayama University
Statistics
Citations: 48
Authors: 9
Affiliations: 4
Identifiers
Doi:
10.1021/jm300887b
ISSN:
00222623
e-ISSN:
15204804