Abstract
A novel series of acyclic pyridine thioglycosides has been synthesized. Evaluation of the anti proliferative activity of these compounds against HEPG-2 cell lines (liver carcinoma cell lines) shows that most of the compounds have high anti-tumor activities especially 6b, 6c, 7b and 7c. Furthermore, in the modeling study, these compounds showed that they have high binding affinity with thymidylate synthase dihydrofolate reductase (TS-DHFR).
Keywords:
Acyclic pyridine thioglycosides; anti-tumor activity; cytotoxic activity; docking studies; thioglycosides; thymidylate synthase dihydrofolate reductase (TS-DHFR).
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / therapeutic use
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Binding Sites
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Carcinoma, Hepatocellular / drug therapy*
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Carcinoma, Hepatocellular / pathology
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Cell Survival / drug effects
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Drug Design
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Hep G2 Cells
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Humans
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Liver Neoplasms / drug therapy*
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Liver Neoplasms / pathology
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Molecular Docking Simulation
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Molecular Structure
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Multienzyme Complexes / metabolism
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Protein Binding
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Pyridines / chemical synthesis*
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Pyridines / therapeutic use
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Structure-Activity Relationship
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Tetrahydrofolate Dehydrogenase / metabolism
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Thioglycosides / chemical synthesis*
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Thioglycosides / therapeutic use
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Thymidylate Synthase / metabolism
Substances
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Antineoplastic Agents
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Multienzyme Complexes
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Pyridines
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Thioglycosides
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thymidylate synthase-dihydrofolate reductase
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Tetrahydrofolate Dehydrogenase
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Thymidylate Synthase