Biological Evaluation of Pyrazinamide Derivatives as An Anticancer Class

Felipe A. R. Rodrigues, Igor da S. Bomfim, Bruno C. Cavalcanti, Claudia do Ó Pessoa, Alessandra C. Pinheiro, Camilo H. S. Lima, Marcus V. N. de Souza


A series of fifty one pyrazinyl derivatives have been synthesized and evaluated for their activity against four cancer cell lines, exhibiting good citotoxicity (IC50 ranging from 1.1 to 5.6μg/mL). The structure-activity relationship (SAR) analysis indicated that the hydroxyl group located in ortho position is critical for the biological activity of these compounds. The presence of hydroxyl groups on benzene ring plays an important role in the anticancer activity of this series, feature especially observed in dissubstituted derivatives.

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