Design, Synthesis, and Bioactivity Assessment of Novel 2-Phenyl Indole Derivatives Incorporating 4-Thiazolidinone-5-carboxylic Acid as Promising Anti-cancer Agents

We conducted a study to create new chemical compounds using indole derivatives, specifically incorporating thiosemicarbazone (8 a-e) and 4-thiozolidinone-5-carboxylic acid (9 a-e) structures. We then tested these compounds against various bacteria and cancer cells. In our antibacterial tests, the compounds showed moderate inhibitory effects on bacterial growth. However, when we examined their effects on cancer cells, we observed specific patterns of activity. Notably, compounds 9 c and 9 d were highly toxic to NCI-H187 cancer cells, while compounds 8 c, 9 b, 9 c, 9 d, and 9 e exhibited moderate inhibitory activity against KB cancer cells. Compound 8 e displayed strong toxicity against MCF-7 cancer cells. When we assessed the toxicity of these compounds on normal Vero cells, we found that compounds 8 e, 9 b, 9 c, 9 d, and 9 e were less toxic compared to ellipticine, a known anticancer drug. These results suggest that these newly synthesized compounds may have potential applications in cancer treatment, and further research is necessary to explore their therapeutic possibilities. Novel 2-phenyl indole derivatives bearing 4-thiazolidinone-5-carboxylic acid moiety, were synthesized, characterized, and biologically evaluated for their in vitro anticancer activities against the human small-cell lung cancer (NCI-H187), human oral cavity cancer (KB) and human breast cancer (MCF-7), as well as for anti-bacterial activities with both Gram-negative and Gram-positive bacterial strains. Compound 9 c and 9 d were found to be better cytotoxicity against NCI-H187cancer cell line as compared to the standard drugs Ellipticine. The thiosemicarbazone indole 8 e was found to be the most potential cytotoxicity against MCF-7 with a lower IC50 than and low toxicity against Vero cell.image