Synthesis of new 7-chloroquinolinyl thioureas and their biological investigation as potential antimalarial and anticancer agents.
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 microM against the D10 strain of Plasmodium falciparum. Lack of cytotoxicity towards HeLa cells indicates selectivity towards parasites.
Mahajan
Aman
A
Department of Chemistry, University of Cape Town, Private Bag, Rondebosh 7701, South Africa.
Yeh
Susan
S
Nell
Margo
M
van Rensburg
Constance E J
CE
Chibale
Kelly
K
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000977:Antiparasitic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002738:Chloroquine / Q000737:chemistry*; D006367:HeLa Cells; D006801:Humans; D015394:Molecular Structure; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship; D013890:Thiourea / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
D000962:Antimalarials; D000977:Antiparasitic Agents; D002738:Chloroquine; D013890:Thiourea