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

2014; Multidisciplinary Digital Publishing Institute; Volume: 19; Issue: 5 Linguagem: Inglês

10.3390/molecules19056651

1433-1373

Luana da Silva Magalhães Forezi, Nathalia Motta de Carvalho Tolentino, Alessandra Mendonça Teles de Souza, Helena Carla Castro, Raquel Carvalho Montenegro, Rafael Ferreira Dantas, Maria da Conceição Ferreira de Oliveira, Floriano Paes Silva, Leilane Barreto, Rommel Mário Rodríguez Burbano, Bárbara Abrahim-Vieira, Riethe De Oliveira, Vı́tor F. Ferreira, Anna C. Cunha, Fernanda da Costa Santos Boechat, Maria de Souza,

Bioactive Compounds and Antitumor Agents

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.