Síntese e avaliação da atividade citotóxica de novas 5-benzilideno-4-tiazolidinonas
From a biological perspective, the 4-thiazolidinones are of great scientific interest due to its chemical properties and the wide spectrum of biological activities such as antimicrobial and anti-tumor, among others. In this communication we aimed the synthesis and evaluation of cytotoxic activity ag...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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Universidade Federal de Mato Grosso do Sul
2010-04-01
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| Series: | Orbital: The Electronic Journal of Chemistry |
| Subjects: | |
| Online Access: | http://www.orbital.ufms.br/index.php/dqi/article/view/199/47 |
| _version_ | 1811269403942060032 |
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| author | Danniel D. Feitoza Maria do D. Rodrigues Alexandre J. S. Góes Antônio J. Alves Silene C. do Nascimento José G. de Lima |
| author_facet | Danniel D. Feitoza Maria do D. Rodrigues Alexandre J. S. Góes Antônio J. Alves Silene C. do Nascimento José G. de Lima |
| author_sort | Danniel D. Feitoza |
| collection | DOAJ |
| description | From a biological perspective, the 4-thiazolidinones are of great scientific interest due to its chemical properties and the wide spectrum of biological activities such as antimicrobial and anti-tumor, among others. In this communication we aimed the synthesis and evaluation of cytotoxic activity against the neoplastic cells of some 5-benzylidene-4-thiazolidinone derivatives obtained from 4-pyridinecarboxaldehyde. The synthesis of the 5-benzylidene-4-thiazolidinone derivatives was performed by Knoevenagel condensation of 4-thiazolidinones and with suitable aromatic aldehydes, using piperidine as base in refluxing ethanol, providing compounds with a good yield ranging from 65% to 77%. The in vitro cytotoxic activity was performed by MTT assay against two human carcinoma cell lines: NCI-H292 (obtained from mucoepidermoid carcinoma of lung) and HEp-2 (obtained from epidermoid carcinoma of the larynx). The tests were conducted at concentrations of 10, 5, 2.5 and 1.25 μg/mL. Among the compounds tested 5-(4-dimethylamino-benzylidene)-4-thiazolidinone showed the best percentage of inhibition of cells with an IC50 of 1.74 μg/mL for cell line NCI-H292. 4-Thiazolidinone compounds come in recent years with increasing attention to the scientific community. In this work we are highlighting the potential of this compound for anti-proliferative activity for NCI-H292 cells. This result is encouraging for further studies of the cytotoxic activity of 4-thiazolidinones. |
| first_indexed | 2024-04-12T21:41:25Z |
| format | Article |
| id | doaj.art-b245ae0292e046ac9a4faaf5d393dea1 |
| institution | Directory Open Access Journal |
| issn | 1984-6428 |
| language | English |
| last_indexed | 2024-04-12T21:41:25Z |
| publishDate | 2010-04-01 |
| publisher | Universidade Federal de Mato Grosso do Sul |
| record_format | Article |
| series | Orbital: The Electronic Journal of Chemistry |
| spelling | doaj.art-b245ae0292e046ac9a4faaf5d393dea12022-12-22T03:15:45ZengUniversidade Federal de Mato Grosso do SulOrbital: The Electronic Journal of Chemistry1984-64282010-04-012Suppl. 1910Síntese e avaliação da atividade citotóxica de novas 5-benzilideno-4-tiazolidinonasDanniel D. FeitozaMaria do D. RodriguesAlexandre J. S. GóesAntônio J. AlvesSilene C. do NascimentoJosé G. de LimaFrom a biological perspective, the 4-thiazolidinones are of great scientific interest due to its chemical properties and the wide spectrum of biological activities such as antimicrobial and anti-tumor, among others. In this communication we aimed the synthesis and evaluation of cytotoxic activity against the neoplastic cells of some 5-benzylidene-4-thiazolidinone derivatives obtained from 4-pyridinecarboxaldehyde. The synthesis of the 5-benzylidene-4-thiazolidinone derivatives was performed by Knoevenagel condensation of 4-thiazolidinones and with suitable aromatic aldehydes, using piperidine as base in refluxing ethanol, providing compounds with a good yield ranging from 65% to 77%. The in vitro cytotoxic activity was performed by MTT assay against two human carcinoma cell lines: NCI-H292 (obtained from mucoepidermoid carcinoma of lung) and HEp-2 (obtained from epidermoid carcinoma of the larynx). The tests were conducted at concentrations of 10, 5, 2.5 and 1.25 μg/mL. Among the compounds tested 5-(4-dimethylamino-benzylidene)-4-thiazolidinone showed the best percentage of inhibition of cells with an IC50 of 1.74 μg/mL for cell line NCI-H292. 4-Thiazolidinone compounds come in recent years with increasing attention to the scientific community. In this work we are highlighting the potential of this compound for anti-proliferative activity for NCI-H292 cells. This result is encouraging for further studies of the cytotoxic activity of 4-thiazolidinones.http://www.orbital.ufms.br/index.php/dqi/article/view/199/474-thiazolidinoneanti-proliferativebenzylidenecytotoxic |
| spellingShingle | Danniel D. Feitoza Maria do D. Rodrigues Alexandre J. S. Góes Antônio J. Alves Silene C. do Nascimento José G. de Lima Síntese e avaliação da atividade citotóxica de novas 5-benzilideno-4-tiazolidinonas Orbital: The Electronic Journal of Chemistry 4-thiazolidinone anti-proliferative benzylidene cytotoxic |
| title | Síntese e avaliação da atividade citotóxica de novas 5-benzilideno-4-tiazolidinonas |
| title_full | Síntese e avaliação da atividade citotóxica de novas 5-benzilideno-4-tiazolidinonas |
| title_fullStr | Síntese e avaliação da atividade citotóxica de novas 5-benzilideno-4-tiazolidinonas |
| title_full_unstemmed | Síntese e avaliação da atividade citotóxica de novas 5-benzilideno-4-tiazolidinonas |
| title_short | Síntese e avaliação da atividade citotóxica de novas 5-benzilideno-4-tiazolidinonas |
| title_sort | sintese e avaliacao da atividade citotoxica de novas 5 benzilideno 4 tiazolidinonas |
| topic | 4-thiazolidinone anti-proliferative benzylidene cytotoxic |
| url | http://www.orbital.ufms.br/index.php/dqi/article/view/199/47 |
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