You are currently viewing a new version of our website. To view the old version click .
Scientia Pharmaceutica
  • Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2016). Previous articles were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence, and they are hosted by MDPI on mdpi.com as a courtesy and upon agreement with Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG).
  • Article
  • Open Access

15 October 2009

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

,
,
,
,
,
,
and
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

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.

Article Metrics

Citations

Article Access Statistics

Multiple requests from the same IP address are counted as one view.