Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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

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, Marcus Vinicius Nora de Souza.

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

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Article Details

VOLUME: 9
ISSUE: 3
Year: 2012
Page: [251 - 256]
Pages: 6
DOI: 10.2174/157018012799129837
Price: $58