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

被引:12
|
作者
Franca, Paulo H. B. [2 ]
Da Silva-Junior, Edeildo F. [2 ]
Aquino, Pedro G. V. [1 ]
Santana, Antonio E. G. [1 ]
Ferro, Jamylle N. S. [3 ]
Barreto, Emiliano De Oliveira [3 ]
Pessoa, Claudia Do O. [4 ]
Meira, Assuero Silva [4 ]
De Aquino, Thiago M. [2 ]
Alexandre-Moreira, Magna S. [5 ]
Schmitt, Martine [6 ]
De Araujo-Junior, Joao X. [2 ]
机构
[1] Univ Fed Alagoas, Inst Chem & Biotechnol, Nat Resources Res Lab, Maceio, Brazil
[2] Univ Fed Alagoas, Sch Nursing & Pharm, Med Chem Lab, Maceio, Brazil
[3] Univ Fed Alagoas, Cell Biol Lab, Biol & Hlth Sci, Maceio, Brazil
[4] Univ Fed Ceara, Dept Physiol & Pharmacol, Expt Oncol Lab, Fortaleza, Ceara, Brazil
[5] Univ Fed Alagoas, Inst Biol & Hlth Sci, Lab Pharmacol & Immun, Maceio, Brazil
[6] Univ Strasbourg, Lab Innovat Therapeut, Fac Pharm, Illkirck, France
关键词
guanylhydrazone; cytotoxic effect; synthesis; MTT assay; INHIBITORS; RECEPTOR;
D O I
10.1515/acph-2016-0015
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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, by 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 mu mol L-1 against four tumor cell lines. Among them, 7 was less toxic to non-tumor cells. Finally, obtained data suggest that guanylhydrazones may be regarded as potential lead compounds for the design of novel anticancer agents.
引用
收藏
页码:129 / 137
页数:9
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