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.
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Authors | Hessa H Al Rasheed, Azizah M Malebari, Kholood A Dahlous, Darren Fayne, Ayman El-Faham |
Journal | Molecules (Basel, Switzerland)
(Molecules)
Vol. 25
Issue 18
(Sep 05 2020)
ISSN: 1420-3049 [Electronic] Switzerland |
PMID | 32899566
(Publication Type: Journal Article)
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Chemical References |
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Topics |
- Apoptosis
(drug effects)
- Cell Proliferation
(drug effects)
- HCT116 Cells
- Humans
- Inhibitory Concentration 50
- MCF-7 Cells
- Molecular Docking Simulation
- Schiff Bases
(chemical synthesis, chemistry, pharmacology)
- Triazines
(chemical synthesis, chemistry, pharmacology)
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