Key result
Novel dihydropyridine and pyridine thioglycosides inhibit HepG-2 liver carcinoma cells via high TS-DHFR binding.
Why the study?
A novel series of dihydropyridine and pyridine thioglycosides was synthesized to evaluate their antitumor activity and binding affinity to TS-DHFR.
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Novel dihydropyridine and pyridine thioglycosides demonstrate promising in vitro anti-proliferative activity against liver carcinoma cells and high binding affinity to TS-DHFR.
A convenient synthesis of a novel series of dihydropyridine and pyridine thioglycosides was developed. The evaluation of anti-proliferative activity against HepG-2 cell lines (liver carcinoma cell lines) shows that most of the compounds have antitumor activity, especially 5b, 5f, 5j, 5n, 7b, 7f, 7j, 7n, 8b, 8f, and 8j. The results of molecular docking reveal that these compounds have high binding affinity by hydrogen bond formation with the binding pocket of thymidylate synthase dihydrofolate reductase (TS-DHFR).
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Elgemeie et al. (2017) studied Liver carcinoma (HepG-2 cell lines). Novel dihydropyridine thioglycosides and pyridine thioglycosides was evaluated on Anti-proliferative activity and binding affinity to TS-DHFR. Novel dihydropyridine and pyridine thioglycosides demonstrated anti-proliferative activity against HepG-2 liver carcinoma cell lines and high binding affinity to TS-DHFR.
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