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Medicinal Chemistry


ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Synthesis and Antitumoral Evaluation of 7-chloro-4-quinolinylhydrazones 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, Laura Nogueira de Faria Cardoso, Carlos Roland Kaiser and Marcus Vinicius Nora de Souza

Volume 7, Issue 6, 2011

Page: [599 - 604] Pages: 6

DOI: 10.2174/157340611797928299

Price: $65


A series of twenty-one 7-chloro-4-quinolinylhydrazones derivatives (3a-u) have been synthesized and evaluated for their cytotoxic potential against three cancer cell lines using MTT assay. The compounds 3b, 3e, 3f, 3h, 3j, 3n, 3r and 3u displayed more than 90% of growth inhibition (GI) and they were selected for in vitro anticancer activities evaluation against four human cancer cell lines. These results were expressed as the concentrations that induce 50% inhibition of cell growth (IC50) in μg/mL. Considering that, compounds 3b, 3e, 3h, 3n, 3r and 3u exhibited good cytotoxic activity against at least three cancer cell lines (0.7967- 4.200 μg/mL). In general, we observed that the presence of electronwithdrawing groups in the benzene ring is important for the anticancer activity in this series, such as fluorine (3h), chlorine (3b) amd bromine (3e) groups in meta position and nitro group (3r) in para position. These derivatives could be considered interesting start points to develop a new anticancer drug and confirm the potential of chloroquine derivatives as lead compounds in anticancer drug discovery.

Keywords: Antitumoral activity, cancer, chloroquine, drugs, quinoline, 7-chloro-4-quinolinylhydrazones derivatives, human cancer cell lines, anticancer drug discovery, chloroquine derivatives

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