Preliminary in vitro evaluation of the anti-proliferative activity of guanylhydrazone derivatives
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)...
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| Format: | Article |
| Language: | English |
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Sciendo
2016-03-01
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| Series: | Acta Pharmaceutica |
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| Online Access: | https://doi.org/10.1515/acph-2016-0015 |
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| author | França Paulo H. B. Da Silva-Júnior Edeildo F. Aquino Pedro G. V. Santana Antônio E. G. Ferro Jamylle N. S. De Oliveira Barreto Emiliano Do Ó Pessoa Cláudia Meira Assuero Silva De Aquino Thiago M. Alexandre-Moreira Magna S. Schmitt Martine De Araújo-Júnior João X. |
| author_facet | França Paulo H. B. Da Silva-Júnior Edeildo F. Aquino Pedro G. V. Santana Antônio E. G. Ferro Jamylle N. S. De Oliveira Barreto Emiliano Do Ó Pessoa Cláudia Meira Assuero Silva De Aquino Thiago M. Alexandre-Moreira Magna S. Schmitt Martine De Araújo-Júnior João X. |
| author_sort | França Paulo H. B. |
| collection | DOAJ |
| description | 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 μmol 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. |
| format | Article |
| id | doaj-art-b26b6c59995d42e684cd8546ec02bcbe |
| institution | Kabale University |
| issn | 1846-9558 |
| language | English |
| publishDate | 2016-03-01 |
| publisher | Sciendo |
| record_format | Article |
| series | Acta Pharmaceutica |
| spelling | doaj-art-b26b6c59995d42e684cd8546ec02bcbe2025-02-02T11:49:55ZengSciendoActa Pharmaceutica1846-95582016-03-0166112913710.1515/acph-2016-0015acph-2016-0015Preliminary in vitro evaluation of the anti-proliferative activity of guanylhydrazone derivativesFrança Paulo H. B.0Da Silva-Júnior Edeildo F.1Aquino Pedro G. V.2Santana Antônio E. G.3Ferro Jamylle N. S.4De Oliveira Barreto Emiliano5Do Ó Pessoa Cláudia6Meira Assuero Silva7De Aquino Thiago M.8Alexandre-Moreira Magna S.9Schmitt Martine10De Araújo-Júnior João X.11 Laboratory of Medicinal Chemistry, School of Nursing and Pharmacy, Federal University of Alagoas, Maceio, Brazil Laboratory of Medicinal Chemistry, School of Nursing and Pharmacy, Federal University of Alagoas, Maceio, Brazil Natural Resources Research Laboratory, Institute of Chemistry and Biotechnology, Federal University of Alagoas, Maceio, Brazil Natural Resources Research Laboratory, Institute of Chemistry and Biotechnology, Federal University of Alagoas, Maceio, Brazil Cell Biology Laboratory, Biological and Health Sciences, Federal University of Alagoas, Maceio, Brazil Cell Biology Laboratory, Biological and Health Sciences, Federal University of Alagoas, Maceio, Brazil Experimental Oncology Laboratory, Department of Physiology and Pharmacology, Federal University of Ceara, Fortaleza, Brazil Experimental Oncology Laboratory, Department of Physiology and Pharmacology, Federal University of Ceara, Fortaleza, Brazil Laboratory of Medicinal Chemistry, School of Nursing and Pharmacy, Federal University of Alagoas, Maceio, Brazil Institute of Biological and Health Sciences, Laboratory of Pharmacology and Immunity, Federal University of Alagoas, Maceio, Brazil Laboratoire d’innovation Thérapeutique, Faculté de Pharmacie, Université de Strasbourg, Illkirck, France Laboratory of Medicinal Chemistry, School of Nursing and Pharmacy, Federal University of Alagoas, Maceio, BrazilGuanylhydrazones 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 μmol 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.https://doi.org/10.1515/acph-2016-0015guanylhydrazonecytotoxic effectsynthesismtt assay |
| spellingShingle | França Paulo H. B. Da Silva-Júnior Edeildo F. Aquino Pedro G. V. Santana Antônio E. G. Ferro Jamylle N. S. De Oliveira Barreto Emiliano Do Ó Pessoa Cláudia Meira Assuero Silva De Aquino Thiago M. Alexandre-Moreira Magna S. Schmitt Martine De Araújo-Júnior João X. Preliminary in vitro evaluation of the anti-proliferative activity of guanylhydrazone derivatives Acta Pharmaceutica guanylhydrazone cytotoxic effect synthesis mtt assay |
| title | Preliminary in vitro evaluation of the anti-proliferative activity of guanylhydrazone derivatives |
| title_full | Preliminary in vitro evaluation of the anti-proliferative activity of guanylhydrazone derivatives |
| title_fullStr | Preliminary in vitro evaluation of the anti-proliferative activity of guanylhydrazone derivatives |
| title_full_unstemmed | Preliminary in vitro evaluation of the anti-proliferative activity of guanylhydrazone derivatives |
| title_short | Preliminary in vitro evaluation of the anti-proliferative activity of guanylhydrazone derivatives |
| title_sort | preliminary in vitro evaluation of the anti proliferative activity of guanylhydrazone derivatives |
| topic | guanylhydrazone cytotoxic effect synthesis mtt assay |
| url | https://doi.org/10.1515/acph-2016-0015 |
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