Synthesis and Antitumoral Evaluation of 7-chloro-4-quinolinylhydrazones Derivatives

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; Marcus      Vinicius Nora de Souza

doi:10.2174/157340611797928299

Abstract

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