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

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,* email
Received: 25 March 2014; in revised form: 1 May 2014 / Accepted: 12 May 2014 / Published: 22 May 2014
(This article belongs to the Section Medicinal Chemistry)
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Abstract: 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
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MDPI and ACS Style

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.

AMA Style

Forezi LSM, Tolentino NMC, de Souza AMT, Castro HC, Montenegro RC, Dantas RF, Oliveira MEIM, Silva, Jr. FP, Barreto LH, Burbano RMR, Abrahim-Vieira B, de Oliveira R, Ferreira VF, Cunha AC, Boechat FCS, de Souza MCBV. Synthesis, Cytotoxicity and Mechanistic Evaluation of 4-Oxoquinoline-3-carboxamide Derivatives: Finding New Potential Anticancer Drugs. Molecules. 2014; 19(5):6651-6670.

Chicago/Turabian Style

Forezi, Luana S.M.; Tolentino, Nathalia M.C.; de Souza, Alessandra M.T.; Castro, Helena C.; Montenegro, Raquel C.; Dantas, Rafael F.; Oliveira, Maria E.I.M.; Silva, Jr., Floriano P.; Barreto, Leilane H.; Burbano, Rommel M.R.; Abrahim-Vieira, Bárbara; de Oliveira, Riethe; Ferreira, Vitor F.; Cunha, Anna C.; Boechat, Fernanda C.S.; de Souza, Maria C.B.V. 2014. "Synthesis, Cytotoxicity and Mechanistic Evaluation of 4-Oxoquinoline-3-carboxamide Derivatives: Finding New Potential Anticancer Drugs." Molecules 19, no. 5: 6651-6670.


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