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Sci. Pharm.
Volume 82
Issue 1
10.3797/scipharm.1307-25
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Short Communication

Biological Evaluation of Isoniazid Derivatives as an Anticancer Class

by
Felipe A. R. RODRIGUES
1,
Augusto C. A. OLIVEIRA
1,
Bruno C. CAVALCANTI
1,
Claudia PESSOA
1,
Alessandra C. PINHEIRO
2 and
Marcus V. N. DE SOUZA
2,*
1
Laboratório de Oncologia Experimental, Universidade Federal do Ceará, Fortaleza, CE, Brazil
2
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.
Sci. Pharm. 2014, 82(1), 21-28; https://doi.org/10.3797/scipharm.1307-25
Submission received: 31 July 2013 / Accepted: 22 September 2013 / Published: 22 September 2013
Versions Notes

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.
Keywords: Antitumor activity; Isoniazid; Hydrazone; Drugs; Cytotoxicity Antitumor activity; Isoniazid; Hydrazone; Drugs; Cytotoxicity

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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. https://doi.org/10.3797/scipharm.1307-25

AMA Style

RODRIGUES FAR, OLIVEIRA ACA, CAVALCANTI BC, PESSOA C, PINHEIRO AC, DE SOUZA MVN. Biological Evaluation of Isoniazid Derivatives as an Anticancer Class. Scientia Pharmaceutica. 2014; 82(1):21-28. https://doi.org/10.3797/scipharm.1307-25

Chicago/Turabian Style

RODRIGUES, Felipe A. R., Augusto C. A. OLIVEIRA, Bruno C. CAVALCANTI, Claudia PESSOA, Alessandra C. PINHEIRO, and Marcus V. N. DE SOUZA. 2014. "Biological Evaluation of Isoniazid Derivatives as an Anticancer Class" Scientia Pharmaceutica 82, no. 1: 21-28. https://doi.org/10.3797/scipharm.1307-25

APA Style

RODRIGUES, F. A. R., OLIVEIRA, A. C. A., CAVALCANTI, B. C., PESSOA, C., PINHEIRO, A. C., & DE SOUZA, M. V. N. (2014). Biological Evaluation of Isoniazid Derivatives as an Anticancer Class. Scientia Pharmaceutica, 82(1), 21-28. https://doi.org/10.3797/scipharm.1307-25

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