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Título: Mefloquine–Oxazolidine derivatives : a new class of anticancer agents
Autor(es): Rodrigues, Felipe A. R.
Bomfim, Igor da S.
Cavalcanti, Bruno C.
Pessoa, Claudia
Goncalves, Raoni S. B.
Wardell, James L.
Wardel, Solange M. S. V.
Souza, Marcus V. N. de
Palavras-chave: Mefloquina
Data do documento: 2014
Editor: 1747-0277
Citação: RODRIGUES, F. A. R. ; BONFIM, I. S. ; CAVALCANTI, B. C. ; PESSOA, C. ; GONÇALVES, R. S. B. ; WARDELL, J. L. ; WARDELL, S. M. S. V. ; SOUZA, M. V. N. (2014)
Abstract: A series of 23 racemic mefloquine–oxazolidine derivatives, 4-[3-(aryl)hexahydro[1,3]oxazolo[3,4-a]pyridin- 1-yl]-2,8-bis(trifluoromethyl)quinolines, derived from (R*, S*)-(±)-mefloquine and arenealdehydes, have been evaluated for their activity against four cancer cell lines (HCT-8, OVCAR-8, HL-60, and SF-295). Good cytotoxicities have been determined with IC50 values ranging from 0.59 to 4.79 lg/mL. In general compounds with aryl groups having strong electron-releasing substituents, such as HO and MeO, or electron-rich heteroaryl groups, for example imidazol-2-y-l, are active. However, other factors such as steric effects may play a role. As both the active and non-active conformations of the mefloquine–oxazolidine derivatives are similar, it is concluded that molecular conformations do not play a significant role either. This study is the first to evaluate mefloquine derivatives as antitumor agents. The mefloquine–oxazolidine derivatives are considered to be useful leads for the rational design of new antitumor agents.
Descrição: RODRIGUES, Felipe A. R. ; BOMFIM, Igor da S. ; CAVALCANTI, Bruno C. ; PESSOA, Claudia ; GONÇALVES, Raoni S. B. ; WARDELL, James L. ; WARDELL, Solange M. S. V. ; SOUZA, Marcus V. N. de. Mefloquine–Oxazolidine derivatives : a new class of anticancer agents. Chemical Biology & Drug Design, Oxford, Inglaterra, v. 83, n. 1, p. 126-131, 2014.
ISSN: 1747-0277
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