Acta Pharm. 66 (2016) 129-137

 

full paper

Short communication

 

Preliminary in vitro evaluation of the anti-proliferative activity of guanylhydrazone derivatives

PAULO H. B. FRANÇA, EDEILDO F. DA SILVA-JÚNIOR, PEDRO G. V. AQUINO, ANTÔNIO E. G. SANTANA, JAMYLLE N. S. FERRO, EMILIANO DE OLIVEIRA BARRETO, CLÁUDIA DO Ó PESSOA, ASSUERO SILVA MEIRA, THIAGO M. DE AQUINO, MAGNA S. ALEXANDRE-MOREIRA, MARTINE SCHMITT and JOÃO X. DE ARAÚJO-JÚNIOR

edeildojr@hotmail.com; jotaaranjo2004@gmail.com

1 Natural Resources Research Laboratory, Institute of Chemistry and Biotechnology, Federal University of Alagoas, Maceio, Brazil

2 Laboratory of Medicinal Chemistry, School of Nursing and Pharmacy, Federal University of Alagoas, Maceio, Brazil

3 Cell Biology Laboratory, Biological and Health Sciences, Federal University of Alagoas, Maceio, Brazil

4 Experimental Oncology Laboratory, Department of Physiology and Pharmacology, Federal University of Ceara, Fortaleza, Brazil

5 Institute of Biological and Health Sciences, Laboratory of Pharmacology and Immunity, Federal University of Alagoas, Maceio, Brazil

6 Laboratoire d’innovation Thérapeutique, Faculté de Pharmacie, Université de Strasbourg, Illkirck, France

Accepted November 25, 2015

 

Guanylhydrazones have shown promising antitumor activity in preclinical tumor models in several studies. In this study, we aimed at evaluating the cytotoxic effect of a series of synthetic guanylhydrazones. Different human tumor cell lines, including HCT-8 (colon carcinoma), MDA-MB-435 (melanoma) and SF-295 (glioblastoma) were continuous exposed to guanylhydrazone derivatives for 72 hours and growth inhibition of tumor cell lines and macrophages J774 was measured using tetrazolium salt (MTT) assay. Compounds 7, 11, 16 and 17 showed strong cytotoxic activity with IC50 values lower than 10 μmol L–1 against four tumor cell lines. Among them, 7 was less toxic to non-tumor cells. Finally, the obtained data suggest that guanylhydrazones may be regarded as potential lead compounds for the design of novel anticancer agents.

 

Keywords: guanylhydrazone, cytotoxic effect, synthesis, MTT assay