Synthesis and anti-proliferative studies of 2-acyl-4-(het)arylthiazoles on human hepatoma cells

We herein report an improved protocol for the synthesis of 2-acyl-4-(het)arylthiazoles by reacting α-oxothioamides with α-bromocarbonyl compounds in acetonitrile under microwave irradiation. One of the thiazoles, (4-(4-bromophenyl)thiazol-2-yl)( m -tolyl)methanone ( SW-07 ) has emerged as the best cytotoxic agent against HepG2 and HCCLM3 liver cancer cells with IC₅₀ values of 6.77 ± 1.10 μM and 7.97 ± 1.15 μM respectively. This lead compound is better than standard drug cisplatin with respect to cytotoxicity. The nuclear fragmentation, chromatin condensation and membrane blebbing enhanced the apoptotic cell death. Further, this lead compound has increased the formation of acidic vesicular organelles and thus enhanced autophagy. • Synthesis of thiazoles. • Anticancer effects on human hepatoma cells. • Cytotoxic studies.