Vol 49, No 3 (2011)
Original paper
Published online: 2011-10-28
The activity of a new 2-amino-1,3,4-thiadiazole derivative 4ClABT in cancer and normal cells
DOI: 10.5603/FHC.2011.0062
Folia Histochem Cytobiol 2011;49(3):436-444.
Abstract
The 2-amino-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole set are well known compounds with interesting
in vitro and in vivo anti-cancer profiles. The aim of this study was an in vitro 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 — chlorophenyl derivative, FABT and 3FABT
— fluorophenyl derivatives and 4BrABT — bromophenyl derivative). The molecular mechanisms and the in
vivo activity of aminothiadiazole derivatives will be the subject of further studies. (Folia Histochemica et Cytobiologica
2011; Vol. 49, No. 3, pp. 436–444)
Keywords: 2-amino-134-thiadiazolecancer and normal cellsanti-cancer activitycell proliferationcell motility
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