The activity of a new 2-amino-1,3,4-thiadiazole derivative 4ClABT in cancer and normal cells
The 2-amino-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole set are well known compounds with interesting <i>in vitro</i> and in vivo anti-cancer profiles. The aim of this study was an <i>in vitro</i> evaluation of the anti-cancer activity of a new s...
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| Format: | Article |
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Via Medica
2011-10-01
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| Series: | Folia Histochemica et Cytobiologica |
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| Online Access: | http://czasopisma.viamedica.pl/fhc/article/view/9438 |
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| author | Andrzej Niewiadomy Joanna Matysiak Małgorzata Juszczak Wojciech Rzeski |
| author_facet | Andrzej Niewiadomy Joanna Matysiak Małgorzata Juszczak Wojciech Rzeski |
| author_sort | Andrzej Niewiadomy |
| collection | DOAJ |
| description | The 2-amino-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole set are well known compounds with interesting <i>in vitro</i> and in vivo anti-cancer profiles. The aim of this study was an <i>in vitro</i> evaluation of the anti-cancer activity of a new synthesized aminothiadiazole derivative 2-(3-chlorophenyloamino)-5-(2,4-dihydroxyphenyl)- -1,3,4-thiadiazole 4ClABT. The effect on tumor cell proliferation, motility and morphology, DNA synthesis as well as the influence on normal cells was assessed. The antiproliferative activity of 4ClABT in tumor cells derived from peripheral cancers including breast carcinoma (T47D), colon carcinoma (HT-29), thyroid carcinoma (FTC-238), teratoma (P19), and T-cell leukemia (Jurkat E6.1), as well as cancers of the nervous system including rhabdomyosarcoma/medulloblastoma (TE671), brain astrocytoma (MOGGCCM) and glioma (C6) was studied by means of MTT assay. DNA synthesis level was determined in BrdU ELISA test. Wound assay model was applied for tumor cell motility assessment. Morphological changes induced by 4ClABT in cancer and normal cells were analyzed in HE staining specimens. Moreover, the influence of 4ClABT on normal cells including skin fibroblasts (HSF), hepatocytes (Fao), astroglia and neurons was studied by means of LDH assay. The tested compound inhibited the proliferation of tumor cells in dose-dependent fashion. The anti-cancer effect was attributed to decreased DNA synthesis, prominent changes in tumor cell morphology as well as reduced cell motility. In antiproliferative concentrations, 4ClABT was not toxic to normal cells. Our study showed prominent anti-cancer effects of the tested aminothiadiazole derivative in the absence of toxicity in normal cells. The obtained results confirmed the promising anti-cancer profile of previously tested 2-(monohalogenphenylamino)- -5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole derivatives (ClABT &#8212; chlorophenyl derivative, FABT and 3FABT &#8212; fluorophenyl derivatives and 4BrABT &#8212; bromophenyl derivative). The molecular mechanisms and the in vivo activity of aminothiadiazole derivatives will be the subject of further studies. (<i>Folia Histochemica et Cytobiologica 2011; Vol. 49, No. 3, pp. 436&#8211;444</i>) |
| first_indexed | 2024-12-21T02:37:29Z |
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| institution | Directory Open Access Journal |
| issn | 0239-8508 1897-5631 |
| language | English |
| last_indexed | 2024-12-21T02:37:29Z |
| publishDate | 2011-10-01 |
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| spelling | doaj.art-b6927f13448e4c0f8e505d11bcd964cc2022-12-21T19:18:46ZengVia MedicaFolia Histochemica et Cytobiologica0239-85081897-56312011-10-0149343644410.5603/9438The activity of a new 2-amino-1,3,4-thiadiazole derivative 4ClABT in cancer and normal cellsAndrzej NiewiadomyJoanna MatysiakMałgorzata JuszczakWojciech RzeskiThe 2-amino-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole set are well known compounds with interesting <i>in vitro</i> and in vivo anti-cancer profiles. The aim of this study was an <i>in vitro</i> evaluation of the anti-cancer activity of a new synthesized aminothiadiazole derivative 2-(3-chlorophenyloamino)-5-(2,4-dihydroxyphenyl)- -1,3,4-thiadiazole 4ClABT. The effect on tumor cell proliferation, motility and morphology, DNA synthesis as well as the influence on normal cells was assessed. The antiproliferative activity of 4ClABT in tumor cells derived from peripheral cancers including breast carcinoma (T47D), colon carcinoma (HT-29), thyroid carcinoma (FTC-238), teratoma (P19), and T-cell leukemia (Jurkat E6.1), as well as cancers of the nervous system including rhabdomyosarcoma/medulloblastoma (TE671), brain astrocytoma (MOGGCCM) and glioma (C6) was studied by means of MTT assay. DNA synthesis level was determined in BrdU ELISA test. Wound assay model was applied for tumor cell motility assessment. Morphological changes induced by 4ClABT in cancer and normal cells were analyzed in HE staining specimens. Moreover, the influence of 4ClABT on normal cells including skin fibroblasts (HSF), hepatocytes (Fao), astroglia and neurons was studied by means of LDH assay. The tested compound inhibited the proliferation of tumor cells in dose-dependent fashion. The anti-cancer effect was attributed to decreased DNA synthesis, prominent changes in tumor cell morphology as well as reduced cell motility. In antiproliferative concentrations, 4ClABT was not toxic to normal cells. Our study showed prominent anti-cancer effects of the tested aminothiadiazole derivative in the absence of toxicity in normal cells. The obtained results confirmed the promising anti-cancer profile of previously tested 2-(monohalogenphenylamino)- -5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole derivatives (ClABT &#8212; chlorophenyl derivative, FABT and 3FABT &#8212; fluorophenyl derivatives and 4BrABT &#8212; bromophenyl derivative). The molecular mechanisms and the in vivo activity of aminothiadiazole derivatives will be the subject of further studies. (<i>Folia Histochemica et Cytobiologica 2011; Vol. 49, No. 3, pp. 436&#8211;444</i>)http://czasopisma.viamedica.pl/fhc/article/view/94382-amino-134-thiadiazolecancer and normal cellsanti-cancer activitycell proliferationcell motility |
| spellingShingle | Andrzej Niewiadomy Joanna Matysiak Małgorzata Juszczak Wojciech Rzeski The activity of a new 2-amino-1,3,4-thiadiazole derivative 4ClABT in cancer and normal cells Folia Histochemica et Cytobiologica 2-amino-1 3 4-thiadiazole cancer and normal cells anti-cancer activity cell proliferation cell motility |
| title | The activity of a new 2-amino-1,3,4-thiadiazole derivative 4ClABT in cancer and normal cells |
| title_full | The activity of a new 2-amino-1,3,4-thiadiazole derivative 4ClABT in cancer and normal cells |
| title_fullStr | The activity of a new 2-amino-1,3,4-thiadiazole derivative 4ClABT in cancer and normal cells |
| title_full_unstemmed | The activity of a new 2-amino-1,3,4-thiadiazole derivative 4ClABT in cancer and normal cells |
| title_short | The activity of a new 2-amino-1,3,4-thiadiazole derivative 4ClABT in cancer and normal cells |
| title_sort | activity of a new 2 amino 1 3 4 thiadiazole derivative 4clabt in cancer and normal cells |
| topic | 2-amino-1 3 4-thiadiazole cancer and normal cells anti-cancer activity cell proliferation cell motility |
| url | http://czasopisma.viamedica.pl/fhc/article/view/9438 |
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