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Abstract
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The novel 4-thiazolidinone derivatives incorporating an adamantane moiety were synthesized in high yields
through the reaction of N-adamantyl-substituted thioureas and dimethyl acetylenedicarboxylate (DMAD) using
an environmentally benign method. These catalyst-free reactions were performed in an ethanol-water mixture at
room temperature, with short reaction times of 3–8 minutes. The in vitro anticancer activity of the target compounds
was evaluated against the A-549 human non-small cell lung cancer (NSCLC) cell line. Among the target
compounds, 2b, 2c, and 2a exhibited promising cytotoxic effects, with IC50 values of 19.07, 32.92, and 63.38
μM, respectively. Additionally, the mechanisms for inhibition of cell growth and induction of apoptotic cell death
were assessed using DAPI and Annexin V-FITC staining. The results indicated that the 4-thiazolidinone derivatives
incorporating an adamantane moiety have significant potential for the development of anticancer
therapeutics.
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