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Scientia Pharmaceutica, Autorenhinweise 2009
 
 
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Volume 77
Issue 4
10.3797/scipharm.0905-07
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Article

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

by
Rosa FERRER
1,
Gricela LOBO
1,
Neira GAMBOA
2,
Juan RODRIGUES
2,3,
Claudia ABRAMJUK
3,
Klaus JUNG
3,
Michael LEIN
3,4 and
Jaime E. CHARRIS
1,*
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.
Sci. Pharm. 2009, 77(4), 725-742; https://doi.org/10.3797/scipharm.0905-07
Submission received: 11 May 2009 / Accepted: 14 October 2009 / Published: 15 October 2009
Versions Notes

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

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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. https://doi.org/10.3797/scipharm.0905-07

AMA Style

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. https://doi.org/10.3797/scipharm.0905-07

Chicago/Turabian Style

FERRER, Rosa, Gricela LOBO, Neira GAMBOA, Juan RODRIGUES, Claudia ABRAMJUK, Klaus JUNG, Michael LEIN, and Jaime E. CHARRIS. 2009. "Synthesis of [(7-Chloroquinolin-4-yl)amino]chalcones: Potential Antimalarial and Anticancer Agents" Scientia Pharmaceutica 77, no. 4: 725-742. https://doi.org/10.3797/scipharm.0905-07

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