Antimetabolites: Design,synthesis, and cytotoxic evaluation of novel dihydropyridine thioglycosides and pyridine thioglycosides |
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| Authors: | Galal H. Elgemeie Nahed M. Fathy Ayman B. Farag Sheikha A. Alkursani |
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| Affiliation: | 1. Chemistry Department, Faculty of Science, Helwan University, Helwan, Cairo, Egypt;2. Photochemistry Department, National Research Centre, Dokki, Cairo, Egypt;3. Ahram Canadian University, Faculty of Pharmacy, Pharmaceutical Chemistry Department, Giza, Egypt;4. Chemistry Department, Girls College of Science, Dammam, Kingdom of Saudi Arabia |
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| Abstract: | 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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| Keywords: | Dihyropyridine thioglycosides pyridine thioglycosides thioglycosides cytotoxic activity docking studies |
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