Abstract:

In anticancer drug research, there is a need for the synthesis of compounds with selective cytotoxicity compared to the drugs in the market. The current study aimed to determine the cytotoxicities of the bis Mannich bases 1-9 towards human oral squamous cell carcinoma (OSCC). Mannich bases showed cytotoxicity in low micromolar in the range of 1.7-27 µM against OSCC cell lines. The compounds 5 with the highest potency selectivity expression (PSE) value (318.1) and 7 with the highest tumor selectivity (TS) values (TS1:11.2, TS2:15.8) showed promising selective cytotoxicity towards cancer cell lines. According to Western blot analysis, representative compound 7 induced the activation of caspase-3 in HSC-2 cells. These results may suggest that the apoptosis pathway may be one of the possible mechanisms of the actions and lead compound 7 can be subjected to further bioassays.

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