Molecules
(May 2014)
Synthesis, Cytotoxicity and Mechanistic Evaluation of 4-Oxoquinoline-3-carboxamide Derivatives: Finding New Potential Anticancer Drugs
Luana da S. M. Forezi,
Nathalia M. C. Tolentino,
Alessandra M. T. de Souza,
Helena C. Castro,
Raquel C. Montenegro,
Rafael F. Dantas,
Maria E. I. M. Oliveira,
Floriano P. Silva, Jr.,
Leilane H. Barreto,
Rommel M. R. Burbano,
Bárbara Abrahim-Vieira,
Riethe de Oliveira,
Vitor F. Ferreira,
Anna C. Cunha,
Fernanda da C. S. Boechat,
Maria Cecília B. V. de Souza
Affiliations
Luana da S. M. Forezi
Outeiro de São João Batista, Fluminense FederalUniversity (UFF), s/n, Niterói 24020141, RJ, Brazil
Nathalia M. C. Tolentino
Outeiro de São João Batista, Fluminense FederalUniversity (UFF), s/n, Niterói 24020141, RJ, Brazil
Alessandra M. T. de Souza
Laboratory of Molecular Modeling & QSAR (ModMolQSAR), Federal University of Rio de Janeiro (UFRJ), Rio de Janeiro 21949-900, RJ, Brazil
Helena C. Castro
LABIEMol, Outeiro de São João Batista, Fluminense Federal University, s/n, Niterói 24020-141, RJ, Brazil
Raquel C. Montenegro
Institute of Biological Sciences, Federal University of Pará, Av. Augusto Corrêa, n.01—Guamá, Belém, 66075-110, Pará, Brazil
Rafael F. Dantas
Laboratory of Biochemistry of Proteins and Peptides, Oswaldo Cruz Institute, FIOCRUZ, Rio de Janeiro 21040-900, RJ, Brazil
Maria E. I. M. Oliveira
Laboratory of Biochemistry of Proteins and Peptides, Oswaldo Cruz Institute, FIOCRUZ, Rio de Janeiro 21040-900, RJ, Brazil
Floriano P. Silva, Jr.
Laboratory of Biochemistry of Proteins and Peptides, Oswaldo Cruz Institute, FIOCRUZ, Rio de Janeiro 21040-900, RJ, Brazil
Leilane H. Barreto
Institute of Biological Sciences, Federal University of Pará, Av. Augusto Corrêa, n.01—Guamá, Belém, 66075-110, Pará, Brazil
Rommel M. R. Burbano
Institute of Biological Sciences, Federal University of Pará, Av. Augusto Corrêa, n.01—Guamá, Belém, 66075-110, Pará, Brazil
Bárbara Abrahim-Vieira
Laboratory of Molecular Modeling & QSAR (ModMolQSAR), Federal University of Rio de Janeiro (UFRJ), Rio de Janeiro 21949-900, RJ, Brazil
Riethe de Oliveira
Laboratory of Molecular Modeling & QSAR (ModMolQSAR), Federal University of Rio de Janeiro (UFRJ), Rio de Janeiro 21949-900, RJ, Brazil
Vitor F. Ferreira
Outeiro de São João Batista, Fluminense FederalUniversity (UFF), s/n, Niterói 24020141, RJ, Brazil
Anna C. Cunha
Outeiro de São João Batista, Fluminense FederalUniversity (UFF), s/n, Niterói 24020141, RJ, Brazil
Fernanda da C. S. Boechat
Outeiro de São João Batista, Fluminense FederalUniversity (UFF), s/n, Niterói 24020141, RJ, Brazil
Maria Cecília B. V. de Souza
Outeiro de São João Batista, Fluminense FederalUniversity (UFF), s/n, Niterói 24020141, RJ, Brazil
DOI
https://doi.org/10.3390/molecules19056651
Journal volume & issue
Vol. 19,
no. 5
Abstract
Read online
As part of a continuing search for new potential anticancer candidates, we describe the synthesis, cytotoxicity and mechanistic evaluation of a series of 4-oxoquinoline-3-carboxamide derivatives as novel anticancer agents. The inhibitory activity of compounds 10–18 was determined against three cancer cell lines using the MTT colorimetric assay. The screening revealed that derivatives 16b and 17b exhibited significant cytotoxic activity against the gastric cancer cell line but was not active against a normal cell line, in contrast to doxorubicin, a standard chemotherapeutic drug in clinical use. Interestingly, no hemolytical activity was observed when the toxicity of 16b and 17b was tested against blood cells. The in silico and in vitro mechanistic evaluation indicated the potential of 16b as a lead for the development of novel anticancer agents against gastric cancer cells.
Keywords
WeChat QR code
Close
