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Título: Design, synthesis and biological evaluation of (E)-2-(2-arylhydrazinyl)quinoxalines, a promising and potent new class of anticancer agents
Autor(es): Rodrigues, Felipe A. R.
Bomfim, Igor da S. B
Cavalcanti, Bruno C.
Pessoa, Claudia do Ó.
Wardell, James L.
Wardell, Solange M. S. V.
Pinheiro, Alessandra C.
Kaiser, Carlos Roland
Nogueira, Thais C. M.
Low, John N.
Gomes, Ligia R.
Souza, Marcus V. N. de
Palavras-chave: Quinoxalinas
Preparações Farmacêuticas
Data do documento: Fev-2014
Editor: Bioorganic & Medicinal Chemistry Letters
Citação: RODRIGUES, F. A. R. ; BONFIM, I. S. ; CAVALCANTI, B. C. ; PESSOA, C. Ó. ; WARDELL, J. L. ; WARDELL, S. M. S. V. ; PINHEIRO, A. C. ; KAISER, C. R. ; NOGUEIRA, T. C. M. ; LOW, J. N. ; GOMES, L. R. ; SOUZA, M. V. N. (2014)
Abstract: A series of forty-seven quinoxaline derivatives, 2-(XYZC6H2CH@N–NH)-quinoxalines, 1, have been synthesized and evaluated for their activity against four cancer cell lines: potent cytotoxicities were found (IC50 ranging from 0.316 to 15.749 lM). The structure–activity relationship (SAR) analysis indicated that the number, the positions and the type of substituents attached to the aromatic ring are critical for biological activity. The activities do not depend on the electronic effects of the substituents nor on the lypophilicities of the molecules. A common feature of active compounds is an ortho-hydroxy group in the phenyl ring. A potential role of these ortho-hydroxy derivatives is as N,N,O-tridentate ligands complexing with a vital metal, such as iron, and thereby preventing proliferation of cells. The most active compound was (1: X,Y = 2,3-(OH)2, Z = H), which displayed a potent cytotoxicity comparable to that of the reference drug doxorubicin.
Descrição: RODRIGUES, Felipe A. R. ; BONFIM, Igor da S. ; CAVALCANTI, Bruno C. ; PESSOA, Claudia do Ó. ; WARDELL, James L. ; WARDELL, Solange M. S. V. ; PINHEIRO, Alessandra C. ; KAISER, Carlos Roland ; NOGUEIRA, Thais C. M. ; LOW, John N. ; GOMES, Ligia R. ; SOUZA, Marcus V. N. de. Design, synthesis and biological evaluation of (E)-2-(2-Arylhydrazinyl)quinoxalines, a promising and potent new class of anticancer agents. Bioorganic & Medicinal Chemistry Letters, New York, US, v. 24, n. 3, p. 934-939, fev. 2014.
ISSN: 0960-894X
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