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Molecules 2014, 19(5), 6651-6670; doi:10.3390/molecules19056651

Synthesis, Cytotoxicity and Mechanistic Evaluation of 4-Oxoquinoline-3-carboxamide Derivatives: Finding New Potential Anticancer Drugs

1, 1, 2, 3, 4, 5, 5, 5, 4, 4, 2, 2, 1, 1, 1 and 1,*
1 Outeiro de São João Batista, Fluminense FederalUniversity (UFF), s/n, Niterói 24020141, RJ, Brazil 2 Laboratory of Molecular Modeling & QSAR (ModMolQSAR), Federal University of Rio de Janeiro (UFRJ), Rio de Janeiro 21949-900, RJ, Brazil 3 LABIEMol, Outeiro de São João Batista, Fluminense Federal University, s/n, Niterói 24020-141, RJ, Brazil 4 Institute of Biological Sciences, Federal University of Pará, Av. Augusto Corrêa, n.01—Guamá, Belém, 66075-110, Pará, Brazil 5 Laboratory of Biochemistry of Proteins and Peptides, Oswaldo Cruz Institute, FIOCRUZ, Rio de Janeiro 21040-900, RJ, Brazil
* Author to whom correspondence should be addressed.
Received: 25 March 2014 / Revised: 1 May 2014 / Accepted: 12 May 2014 / Published: 22 May 2014
(This article belongs to the Section Medicinal Chemistry)
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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 1018 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: 4-oxoquinoline; carboxamide; heterocycles; anticancer 4-oxoquinoline; carboxamide; heterocycles; anticancer
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Forezi, L.S.M.; Tolentino, N.M.C.; de Souza, A.M.T.; Castro, H.C.; Montenegro, R.C.; Dantas, R.F.; Oliveira, M.E.I.M.; Silva, Jr., F.P.; Barreto, L.H.; Burbano, R.M.R.; Abrahim-Vieira, B.; de Oliveira, R.; Ferreira, V.F.; Cunha, A.C.; Boechat, F.C.S.; de Souza, M.C.B.V. Synthesis, Cytotoxicity and Mechanistic Evaluation of 4-Oxoquinoline-3-carboxamide Derivatives: Finding New Potential Anticancer Drugs. Molecules 2014, 19, 6651-6670.

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