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

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ID: 61376
2014
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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 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.
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Authors Forezi, Luana da S. M.;Tolentino, Nathalia M. C.;Souza, Alessandra M. T. de;Castro, Helena C.;Montenegro, Raquel C.;Dantas, Rafael F.;Oliveira, Maria E. I. M.;Jr., Floriano P. Silva,;Barreto, Leilane H.;Burbano, Rommel M. R.;Abrahim-Vieira, Bárbara;Oliveira, Riethe de;Ferreira, Vitor F.;Cunha, Anna C.;Boechat, Fernanda da C. S.;Souza, Maria Cecília B. V. de;
Journal molecules
Year 2014
DOI
DOI not found
URL
http://www.mdpi.com/1420-3049/19/5/6651
Keywords
chemistry Organic Chemistry Medicine Materials of engineering and construction. Mechanics of materials Technology Science

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