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Antineoplastic activity in vitro of 2-amino-5-benzylthiazole derivative in complex with nanoscale polymeric carriers
SUMMARY. The main problems of modern cancer chemotherapy are the low efficiency and selectivity of anticancer drugs, the development of multi-drug resistance, and low solubility in water. The polymeric nanoscale carriers are widely used to improve the targeted delivery of drugs and to increase their solubility. Earlier, we found that the newly synthesized thiazole derivative (N-(5-benzyl-1,3-thiazol-2-yl) -3,5-dimethyl-1-benzofuran-2-carboxamide, BF1) possessed toxicity towards some tumor line cells. The aim of our work was to investigate the action of BF1 complexed with the polymeric carriers, containing polyethylene glycol (PEG). The investigated complexes exhibited higher cytotoxicity towards specific tumor cell lines compared with the effects of the thiazole derivative or/and doxorubicin (positive control). Ñomplexes 4, 14 and 8, 18 were the most toxic for HepG2 human hepatocarcinoma cells and C6 rat glioma cells. Complex 6 demonstrated high toxicity towards T98G human glioblastoma cells and HL-60 human promyelocytic leukemia cells. Thus, complexes 4, 14 based on the poly(VEP-cî-GMA)-graft-mPEG, complex 6 based on the poly(PEGÌÀ), and complexes 8, 18 based on the poly(PEGMA-co-DMM) selectively enhanced the cytotoxic action of the thiazole derivative BF1 delivered to tumor cells.
Key words: nanoscale polymeric carriers, polyethylene glycol, thiazole derivative, cytotoxic action, antitumor activity, hepatocarcinoma, glioma, leukemia
E-mail: nataliyafiniuk gmail.com, popovych.marta gmail.com, yarunash gmail.com, manisvit gmail.com, grenuh gmail.com, y.ostapiuk gmail.com, obushak in.lviv.ua, nmitina10 gmail.com, zaichenk polynet.lviv.ua, stoika cellbiol.lviv.ua, andriy.babsky gmail.com
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