Synthesis of new 7-chloroquinolinyl thioureas and their biological investigation as potential antimalarial and anticancer agents

Novel 7-chloroquinolinyl thiourea derivatives derived from the corresponding 4,7-dichloroquinoline isothiocyanate were synthesized and evaluated for in vitro antimalarial and anticancer activity. The most active compound from the series displayed an inhibitory IC 50 value of 1.2 μM against the D10 s...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2007-10, Vol.17 (20), p.5683-5685
Main Authors: Mahajan, Aman, Yeh, Susan, Nell, Margo, van Rensburg, Constance E.J., Chibale, Kelly
Format: Article
Language:English
Subjects:
4-Quinolyl isothiocyanate
7-Chloroquinolinyl thioureas
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antimalarials - chemical synthesis
Antimalarials - chemistry
Antimalarials - pharmacology
Antineoplastic agents
Antiparasitic agents
Antiparasitic Agents - chemical synthesis
Antiparasitic Agents - chemistry
Antiparasitic Agents - pharmacology
Biological and medical sciences
Chloroquine - chemistry
General aspects
HeLa Cells
Human adenocarcinoma of the cervix
Humans
Medical sciences
Molecular Structure
Pharmacology. Drug treatments
Plasmodium falciparum
Plasmodium falciparum - drug effects
Structure-Activity Relationship
Thiourea - chemical synthesis
Thiourea - chemistry
Thiourea - pharmacology
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Summary:Novel 7-chloroquinolinyl thiourea derivatives derived from the corresponding 4,7-dichloroquinoline isothiocyanate were synthesized and evaluated for in vitro antimalarial and anticancer activity. The most active compound from the series displayed an inhibitory IC 50 value of 1.2 μM against the D10 strain of Plasmodium falciparum. New 7-chloroquinolinyl thiourea derivatives derived from the corresponding 4,7-dichloroquinoline isothiocyanate were synthesized and evaluated for in vitro antimalarial and anticancer activity. The most active compound from the series displayed an inhibitory IC 50 value of 1.2 μM against the D10 strain of Plasmodium falciparum. Lack of cytotoxicity towards HeLa cells indicates selectivity towards parasites.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.07.049