title: Biological evaluation of isoniazid derivatives as an anticancer class.
abstract: A series of thirty-two isoniazid derivatives have been evaluated for their activity against four human cancer cell lines with potent cytotoxicity (IC50 ranging from 0.61 to 3.36 μg/mL). The structure-activity relationship (SAR) analysis indicated the number, the positions, and the types of substituents attached to the aromatic ring as being critical factors for the biological activity. Briefly, we observed that the presence of a hydroxyl group on the benzene ring plays an important role in the anticancer activity of this series, especially when it is located in ortho-position. Among the thirty-two compounds, three displayed good cytotoxic activity when compared to the reference drug doxorubicin and are thus being considered leading compounds of this new class.
authors.affiliation: Laboratório de Oncologia Experimental, Universidade Federal do Ceará, Fortaleza, CE, Brazil.
authors.forename: Felipe A R
authors.initials: FA
authors.lastname: Rodrigues
authors.affiliation: Laboratório de Oncologia Experimental, Universidade Federal do Ceará, Fortaleza, CE, Brazil.
authors.forename: Augusto C A
authors.initials: AC
authors.lastname: Oliveira
authors.affiliation: Laboratório de Oncologia Experimental, Universidade Federal do Ceará, Fortaleza, CE, Brazil.
authors.forename: Bruno C
authors.initials: BC
authors.lastname: Cavalcanti
authors.affiliation: Laboratório de Oncologia Experimental, Universidade Federal do Ceará, Fortaleza, CE, Brazil.
authors.forename: Claudia
authors.initials: C
authors.lastname: Pessoa
authors.affiliation: FioCruz-Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far-Manguinhos, Rua Sizenando Nabuco, 100, Manguinhos, 21041-250 Rio de Janeiro, RJ, Brazil.
authors.forename: Alessandra C
authors.initials: AC
authors.lastname: Pinheiro
authors.affiliation: FioCruz-Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far-Manguinhos, Rua Sizenando Nabuco, 100, Manguinhos, 21041-250 Rio de Janeiro, RJ, Brazil.
authors.forename: Marcus V N
authors.initials: MV
authors.lastname: de Souza
keywords: Antitumor activity; Cytotoxicity; Drugs; Hydrazone; Isoniazid