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The activity of a new 2-amino-1,3,4-thiadiazole derivative 4ClABT in cancer and normal cells

Author(s): Małgorzata Juszczak | Joanna Matysiak | Andrzej Niewiadomy | Wojciech Rzeski

Journal: Folia Histochemica et Cytobiologica
ISSN 0239-8508

Volume: 49;
Issue: 3;
Start page: 436;
Date: 2011;
Original page

The 2-amino-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole set are well known compounds with interestingin vitro and in vivo anti-cancer profiles. The aim of this study was an in vitro evaluation of the anti-canceractivity 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 aswell as the influence on normal cells was assessed. The antiproliferative activity of 4ClABT in tumor cells derivedfrom 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 includingrhabdomyosarcoma/medulloblastoma (TE671), brain astrocytoma (MOGGCCM) and glioma (C6) was studiedby means of MTT assay. DNA synthesis level was determined in BrdU ELISA test. Wound assay model wasapplied for tumor cell motility assessment. Morphological changes induced by 4ClABT in cancer and normalcells were analyzed in HE staining specimens. Moreover, the influence of 4ClABT on normal cells includingskin fibroblasts (HSF), hepatocytes (Fao), astroglia and neurons was studied by means of LDH assay. The testedcompound inhibited the proliferation of tumor cells in dose-dependent fashion. The anti-cancer effect was attributedto decreased DNA synthesis, prominent changes in tumor cell morphology as well as reduced cellmotility. In antiproliferative concentrations, 4ClABT was not toxic to normal cells. Our study showed prominentanti-cancer effects of the tested aminothiadiazole derivative in the absence of toxicity in normal cells. The obtainedresults confirmed the promising anti-cancer profile of previously tested 2-(monohalogenphenylamino)--5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole derivatives (ClABT — chlorophenyl derivative, FABT and 3FABT— fluorophenyl derivatives and 4BrABT — bromophenyl derivative). The molecular mechanisms and the invivo activity of aminothiadiazole derivatives will be the subject of further studies. (Folia Histochemica et Cytobiologica2011; Vol. 49, No. 3, pp. 436–444)
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