Thiazole conjugated amino acid derivatives as potent cytotoxic agents

Abstract

In the search for anticancer agents, molecular hybridization has gained increasing attention due to its unique advantages like enhanced pharmacological activity, reduced toxicity, and circumvention of drug resistances. In this study, by incorporating amino acids into the thiazole heterocycle scaffold, thirty thiazole–amino acid hybrid derivatives have been successfully synthesized and tested for cytotoxicity against the three human cancer cell lines including lung cancer (A549), cervical cancer (HeLa), and breast cancer (MCF-7) cell lines. The results showed that most of the synthesized hybrid thiazole–amino acids exhibited moderate to good cytotoxicity towards the tested cancer cell lines. Notably, five compounds displayed good cytotoxicity with low IC₅₀ values (2.07–8.51 μM) compared to the positive control 5-fluorouracil (IC₅₀ = 3.49–8.74 μM). These novel thiazole conjugated amino acid derivatives could be considered as lead compounds that merit further optimization and development of anticancer agents.