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Scientia Pharmaceutica, Autorenhinweise 2009
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Sci. Pharm. 2009, 77(4), 725-742; doi:10.3797/scipharm.0905-07

Synthesis of [(7-Chloroquinolin-4-yl)amino]chalcones: Potential Antimalarial and Anticancer Agents

1
Laboratorio de Síntesis Orgánica, Facultad de Farmacia, Universidad Central de Venezuela, Apartado 47206, Los Chaguaramos, 1041-A Caracas, Venezuela
2
Laboratorio de Bioquímica, Facultad de Farmacia, Universidad Central de Venezuela, Apartado 47206, Los Chaguaramos, 1041-A Caracas, Venezuela
3
Department of Urology, University Hospital Charité, Humboldt University, Berlin, Germany
4
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.
Keywords: Malaria; CQ; β-Hematin; Cancer; Prostate Malaria; CQ; β-Hematin; Cancer; Prostate
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

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.

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