Authors: Montenegro, R.C.; Lotufo, L.V.; Moraes, M.O.; Pessoa, C.O.; Rodrigues, F.A.R.; Pinheiro, A.C.; Nogueira, T.C.M.; De Souza, M.V.N.
Source: Letters in Drug Design & Discovery, v. 9, p. 251-256, 2012.
Publisher: Bentham Science
Abstract
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 Document Type: Research Article DOI: http://dx.doi.org/10.2174/157018012799129837 Publication date: 1 de Janeiro de 2012
