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Cytotoxic Activity of Polysubstituted 7-chloro-4-quinolinylhydrazone Derivatives

2012; Bentham Science Publishers; Volume: 9; Issue: 3 Linguagem: Inglês

10.2174/157018012799129837

1875-628X

Raquel Carvalho Montenegro, Letícia V. Costa‐Lotufo, Manoel Odorico de Moraes, Cláudia Pessoa, Felipe Augusto Rocha Rodrigues, Marcelle de Lima Ferreira Bispo, Bruna Abreu Freire, Carlos R. Kaiser, M.V.N. De Souza,

Synthesis and Reactions of Organic Compounds

A series of fourteen polysubstituted 7-chloro-4-quinolinylhydrazone derivatives (3a-n) has been synthesized and evaluated for their activity against four cancer cell lines. Among them, compounds 3a, 3c, 3h, 3i, 3j and 3n showed good cytotoxicity (with IC50 ranging from 0.7483 to 5.572 μg/mL). In general, we observed that the presence of methoxy groups on benzene ring plays an important role in the anticancer activity of this series, especially when they are located in 3,4 (3h) or 3,4,5 (3j) positions. These derivatives could be considered a relevant finding towards the rational design of new leads for antitumoral agents. Keywords: Antitumor activity, Chloroquine, Drugs, Hydrazones, Quinoline, World Health Organization (WHO), quinoline derivatives, CQ, synthetic route, benzene ring, Buchi apparatus, Chemical shifts, Waters mass spectrometer, Cell Membrane Disruption, Cytotoxicity