Synthesis, Molecular Docking and Anticancer Activity of New Pyridyl-1,2,4-Triazole-Thioglycosides and Their Pyridyl-[1,2,4]triazolo[1,5-a]pyridine-Glycoside Analogues

Document Type : Original Article

Authors

1 Department of Chemistry, College of Science, Qassim University, Buraidah 51452, Saudi Arabia

2 Department of Photochemistry, National Research Centre, Cairo 12622, Egypt.

3 Department of Chemistry, Faculty of Science, Islamic University of Madinah, Madinah, 42351, Saudi Arabia

4 Department of Pharmaceutical Medicinal Chemistry and Drug Design, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo 11754, Egypt.

Abstract

Cancer remains a main threat for human life and requires intensive research for discovering and developing treatment strategies. The design and synthesis of novel functionalized and hybrid structures as candidates for anticancer activity investigation have been proven in the literature as an efficient approach for providing a variety of compounds. In the current work, new compounds of hybrid structures incorporating aryl- or heteroarylpyridine, 1,2,4-triazole, glycosyl moieties have been prepared via a stepwise pathway starting from simple available starting compounds. The anticancer activity against MCf-7, PC3 and A549 human cancer cell lines revealed that substituted 1,2,4-triazole-thiol based substituted pyridine structure and the N-glycosyl derivative of the 1,2,4-triazolopyridine compounds exhibited the most potent activities against MCF-7 and A549 cancer cells. Molecular docking into EGFR active site and showed good binding affinities via various modes.

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Volume 67, Issue 13 - Serial Number 13
In Loving Memory of Late Professor Doctor ””Mohamed Refaat Hussein Mahran””
December 2024
Pages 1251-1260
  • Receive Date: 14 October 2024
  • Revise Date: 12 November 2024
  • Accept Date: 25 November 2024