Synthesis and anticancer properties of N-(5-R-benzyl-1,3-thiazol-2-yl)-2,5-dimethyl-3-furamides

Aim. Study of the synthesis and anticancer activity of a series of N-(5-R-benzyl-1,3-thiazol-2-yl)-2,5-dimethyl-3-furamides. Methods. Organic synthesis, analytical and spectral methods, pharmacological screening. Results. N-(5-R-benzyl-1,3-thiazol-2-yl)-2,5-dimethyl-3-furamides 7a-g have been prepared in good yields by the reaction of 2-amino-5-(R-benzyl)thiazoles with 2,5-dimethyl-3-furoylchloride. Their structure was confirmed by 1H NMR spectroscopy and microanalyses. The synthesized compounds have been evaluated for their anticancer activity against 60 cancer lines in the concentration of 10 µM. The human tumour cell lines were derived from nine different cancer types: leukemia, melanoma, lung, colon, CNS, ovarian, renal, prostate, and breast cancers. It was found that compounds 7d,e,g exhibit a high activity with GP = 29.05–35.02 % whereas 7a-c,f – moderate activity with GP = 60.31–67.36 %. The most active compound 7g showed a high inhibition activity (GI50