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Sci. Pharm. 2009, 77(4), 725-742; https://doi.org/10.3797/scipharm.0905-07 (registering DOI)
Synthesis of [(7-Chloroquinolin-4-yl)amino]chalcones: Potential Antimalarial and Anticancer Agents
Laboratorio de Síntesis Orgánica, Facultad de Farmacia, Universidad Central de Venezuela, Apartado 47206, Los Chaguaramos, 1041-A Caracas, Venezuela
Laboratorio de Bioquímica, Facultad de Farmacia, Universidad Central de Venezuela, Apartado 47206, Los Chaguaramos, 1041-A Caracas, Venezuela
Department of Urology, University Hospital Charité, Humboldt University, Berlin, Germany
Berlin Institute for Urologic Research, Berlin, Germany
Author to whom correspondence should be addressed.
Received: 11 May 2009 / Accepted: 14 October 2009 / Published: 15 October 2009
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Abstract [(7-Chloroquinolin-4-yl)amino]chalcone derivatives derived from the corresponding 3- or 4-[(7-chloroquinolin-4-yl)amino]acetophenone were synthesized and evaluated for in vitro antimalarial and anticancer activity. The most active compounds 12, 13, 15, 17 and 19 from the 3-substituted series displayed inhibitory values against heme cristallization in the range of 93.14 ± 1.74 – 94.93 ± 1.50 % as an antimalarial mechanism and cytotoxic effect with IC50 values of 7.93 ± 2.05, 7.11 ± 2.06 and 6.95 ± 1.62 μg/mL for 13, 17 and 19 respectively against humane prostate LNCaP tumor cells.
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FERRER, R.; LOBO, G.; GAMBOA, N.; RODRIGUES, J.; ABRAMJUK, C.; JUNG, K.; LEIN, M.; CHARRIS, J.E. Synthesis of [(7-Chloroquinolin-4-yl)amino]chalcones: Potential Antimalarial and Anticancer Agents. Sci. Pharm. 2009, 77, 725-742.
FERRER R, LOBO G, GAMBOA N, RODRIGUES J, ABRAMJUK C, JUNG K, LEIN M, CHARRIS JE. Synthesis of [(7-Chloroquinolin-4-yl)amino]chalcones: Potential Antimalarial and Anticancer Agents. Scientia Pharmaceutica. 2009; 77(4):725-742.
FERRER, Rosa; LOBO, Gricela; GAMBOA, Neira; RODRIGUES, Juan; ABRAMJUK, Claudia; JUNG, Klaus; LEIN, Michael; CHARRIS, Jaime E. 2009. "Synthesis of [(7-Chloroquinolin-4-yl)amino]chalcones: Potential Antimalarial and Anticancer Agents." Sci. Pharm. 77, no. 4: 725-742.
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