Abstract
Based on the use ofs-triazine as a scaffold, we report here a new series ofs-triazine Schiff base derivatives and their anti-proliferative activity against two cancer cell lines: human breast carcinoma (MCF-7), and colon cancer (HCT-116) compared with tamoxifen as a reference compound. Several derivatives exhibited growth inhibition activity in the sub-micromolar range. The results reveal that thes-triazine Schiff base derivatives showed varied activities and that the substituents on thes-triazine core have a great effect on the anti-proliferative activity. Compounds with a piperidino and benzylamino substituent on thes-triazine moiety4band4cwere most effective in both cell lines compared to the reference compound used. In addition, compound4bhas aparachlorine atom on the benzylidine residue, demonstrating the most potent activity with IC(50)values of 3.29 and 3.64 mu M in MCF-7 and HCT-116, respectively. These results indicate that in general, the nature of the substituents on the triazine core and the type of substituent on the benzilyldene ring significantly influenced the anti-proliferative activity. The results obtained from the anti-proliferative activity and the molecular docking study indicate thats-triazine-hydrazone derivatives may be an excellent scaffold for the development of new anti-cancer agents.