Abstract
Based on the use of s-triazine as a scaffold, we report here a new series of s-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 the s-triazine Schiff base derivatives showed varied activities and that the substituents on the s-triazine core have a great effect on the anti-proliferative activity. Compounds with a piperidino and benzylamino substituent on the s-triazine moiety 4b and 4c were most effective in both cell lines compared to the reference compound used. In addition, compound 4b has a para chlorine atom on the benzylidine residue, demonstrating the most potent activity with IC50 values of 3.29 and 3.64 µM 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 that s-triazine-hydrazone derivatives may be an excellent scaffold for the development of new anti-cancer agents.
Highlights
After cardiovascular diseases, cancer is the second most common cause of death globally, and its occurrence is predicted to increase dramatically in the near future
[30,31,32], we report a new series against breast cancer cells (MCF-7) and colon cancer (HCT-116) [30,31,32], we report a new series of of Schiff
The target compounds 4a-r were synthesized as illustrated in Scheme 1 following the reported
Summary
Cancer is the second most common cause of death globally, and its occurrence is predicted to increase dramatically in the near future. Hydrazine or primary amines and carbonyl compounds to form azomethine type compounds and are considered to considered be importantto derivatives with biological, medicinal, clinical, pharmacological and and are be important derivatives with biological, medicinal, clinical, analytical applications [18,19,20,21]. They are popular ligand precursors due to their versatility pharmacological and analytical applications [18,19,20,21]. They are popular ligand precursors and of preparation
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