Paper
Synthesis of [(7-Chloroquinolin-4-yl)amino]chalcones: Potential Antimalarial and Anticancer Agents
Published Oct 14, 2009 · Rosa Ferrer, G. Lobo, N. Gamboa
Scientia Pharmaceutica
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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.
[(7-Chloroquinolin-4-yl)amino]chalcone derivatives show potential as antimalarial and anticancer agents, with compounds 12, 13, 15, 17, and 19 showing high inhibitory effects against heme crystallization and cytotoxic effects against human prostate LNCaP tumor
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