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Antineoplastic activity in vitro of 2-amino-5-benzylthiazole derivative in complex with nanoscale polymeric carriers

Finiuk N.S., Popovych M.V., Shalai Ya.R., Mandzynets S.M., Grenyukh V.P., Ostapiuk Yu.V., Obushak M.D., Mitina N.E., Zaichenko O.S., Stoika R.S., Babsky A.M.


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). omplexes 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-c-GMA)-graft-mPEG, complex 6 based on the poly(PEG), 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

Tsitologiya i Genetika 2021, vol. 55, no. 1, pp. 23-32

  1. Ivan Franko National University of Lviv, Faculty
    of Biology, Hrushevskoho str., 4, Lviv, 79005, Ukraine
  2. Institute of Cell Biology, NAS of Ukraine, Drahomanov str., 14/16, Lviv, 79005, Ukraine
  3. Ivan Franko National University of Lviv, Faculty of Chemistry, Kyryla i Mefodiya str., 6/8, Lviv, 79005, Ukraine
  4. Lviv Polytechnic National University, Faculty of Chemistry, St. Georges square, 9, Lviv, 79013, Ukraine

E-mail: nataliyafiniuk, popovych.marta, yarunash, manisvit, grenuh, y.ostapiuk, obushak, nmitina10, zaichenk, stoika, andriy.babsky

Finiuk N.S., Popovych M.V., Shalai Ya.R., Mandzynets S.M., Grenyukh V.P., Ostapiuk Yu.V., Obushak M.D., Mitina N.E., Zaichenko O.S., Stoika R.S., Babsky A.M. Antineoplastic activity in vitro of 2-amino-5-benzylthiazole derivative in complex with nanoscale polymeric carriers, Tsitol Genet., 2021, vol. 55, no. 1, pp. 23-32.

In "Cytology and Genetics":
N. S. Finiuk, M. V. Popovych, Ya. R. Shalai, S. M. Mandzynets, V. P. Hreniuh, Yu. V. Ostapiuk, M. D. Obushak, N. E. Mitina, O. S. Zaichenko, R. S. Stoika & A. M. Babsky Antineoplastic Activity In Vitro of 2-amino-5-benzylthiasol Derivative in the Complex with Nanoscale Polymeric Carriers, Cytol Genet., 2021, vol. 55, no. 1, pp. 1927
DOI: 10.3103/S0095452721010084


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