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Sci. Pharm. 2014, 82(1), 21-28; doi:10.3797/scipharm.1307-25 (registering DOI)

Biological Evaluation of Isoniazid Derivatives as an Anticancer Class

Laboratório de Oncologia Experimental, Universidade Federal do Ceará, Fortaleza, CE, Brazil
FioCruz-Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far-Manguinhos, Rua Sizenando Nabuco, 100, Manguinhos, 21041-250 Rio de Janeiro, RJ, Brazil
Author to whom correspondence should be addressed.
Received: 31 July 2013 / Accepted: 22 September 2013 / Published: 22 September 2013
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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.
Keywords: Antitumor activity; Isoniazid; Hydrazone; Drugs; Cytotoxicity Antitumor activity; Isoniazid; Hydrazone; Drugs; Cytotoxicity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

RODRIGUES, F.A.R.; OLIVEIRA, A.C.A.; CAVALCANTI, B.C.; PESSOA, C.; PINHEIRO, A.C.; DE SOUZA, M.V.N. Biological Evaluation of Isoniazid Derivatives as an Anticancer Class. Sci. Pharm. 2014, 82, 21-28.

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