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
Letters in Drug Design & Discovery
Title: Cytotoxic Activity of Polysubstituted 7-chloro-4-quinolinylhydrazone Derivatives
Volume: 9 Issue: 3
Author(s): Raquel Carvalho Montenegro, Leticia Veras Lotufo, Manoel Odorico de Moraes, Claudia do O Pessoa, Felipe Augusto Rocha Rodrigues, Marcelle de Lima Ferreira Bispo, Bruna Abreu Freire, Carlos Roland Kaiser and Marcus Vinicius Nora de Souza
Affiliation:
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
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.
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Carvalho Montenegro Raquel, Veras Lotufo Leticia, Odorico de Moraes Manoel, do O Pessoa Claudia, Augusto Rocha Rodrigues Felipe, de Lima Ferreira Bispo Marcelle, Abreu Freire Bruna, Roland Kaiser Carlos and Vinicius Nora de Souza Marcus, Cytotoxic Activity of Polysubstituted 7-chloro-4-quinolinylhydrazone Derivatives, Letters in Drug Design & Discovery 2012; 9 (3) . https://dx.doi.org/10.2174/157018012799129837
DOI https://dx.doi.org/10.2174/157018012799129837 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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