Journal
JOURNAL OF INORGANIC BIOCHEMISTRY
Volume 105, Issue 7, Pages 985-990Publisher
ELSEVIER SCIENCE INC
DOI: 10.1016/j.jinorgbio.2011.03.019
Keywords
Bioorganometallic chemistry; Chromium; Antimalarial; Chloroquine
Funding
- Swedish International Development Cooperation Agency (SIDA)
- Swedish Research Council (VR)
- SIDA/NRF
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Organometallic analogs of chloroquine (CQ) are of interest as drug candidates that may be able to overcome the widespread chloroquine resistance developed by malaria parasites. Two new chromium arene CQ-analogs: [eta(6)-N-(7-chloroquinolin-4-yl)-N'-(2-dimethylamino-methylbenzyl)-ethane-1,2-diamine]tricarbonylchromium 4 and [eta(6)-N-(7-chloroquinolin-4-yl)-N'-(2-dimethylaminobenzyl)-ethane-1,2-diamine]tricarbonylchromium 9 have been synthesized and characterized. In addition, X-ray crystal structures of the intermediates (eta(6)-benzyldimethylamine)tricarbonylchromium 2, [eta(6)-2-((dimethylamino)methyl) benzaldehyde]tricarbonylchromium 3 and p-(eta(6)-dimethylaminobenzaldehyde)tricarbonyl chromium 8 are reported. Compound 4 was more active than chloroquine against both CQ-sensitive and CQ-resistant strains of Plasmodium falciparum when antimalarial activity was tested in vitro. The activity of 4 against the CQ-resistant parasite strain was twice as high as for the organic ligand alone (IC50 values of 33.9 nM versus 63.1 nM). (C) 2011 Published by Elsevier Inc.
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