Antineoplastic Activity In Vitro of 2-amino-5-benzylthiasol Derivative in the Complex with Nanoscale Polymeric Carriers

Abstract

The main problems of contemporary chemotherapy are the insufficient efficacy of antitumor drugs and low selectivity of their action, development of multidrug resistance, and poor water solubility of antitumor drugs. One of the ways to improve the targeted delivery of drugs and increase their solubility is the use of polymeric nanoscale carriers. The newly synthesized thiazole derivative (N-(5-benzyl-1,3-thiazol-2-yl)-3,5-dimethyl-1-benzofuran-2-carboxamide, BF1) is cytotoxic in its activity towards some tumor cell lines. The aim of this study was to investigate the action of BF1 conjugated with novel polymeric carriers based on polyethylene glycol (PEG). The synthesized complexes exhibited a higher level of cytotoxicity towards specific tumor cell lines than the pure (unconjugated) thiazole derivative or/and doxorubicin (positive control). Complexes 4, 14 and 8, 18 were the most toxic to the human hepatocarcinoma HepG2 and the rat glioma C6 cell lines. Complex 6 exhibited a high level of toxicity towards human glioblastoma T98G and human promyelocytic leukemia HL-60 cell lines. Thus, complexes 4 and 14 based on poly(VEP-co-GMA)-graft-mPEG, complex 6 based on poly(PEGMA), and complexes 8 and 18 based on poly(PEGMA-co-DMM) selectively increase the toxic action of thiazole derivative BF1 towards tumor cells.