Literature DB >> 30864522

Synthesis, Docking Studies into CDK-2 and Anticancer Activity of New Derivatives Based Pyrimidine Scaffold and Their Derived Glycosides.

Adel A H Abdel Rahman1, Ibrahim F Nassar2, Amira K F Shaban1, Dina S El-Kady3, Hanem M Awad4, Wael A El Sayed5,6.   

Abstract

BACKGROUND &
OBJECTIVE: New diaryl-substituted pyrimidinedione compounds, their thioxo derivatives as well as their bicyclic thiazole compounds were synthesized and characterized.
METHODS: The glycosylamino derivatives of the synthesized disubstituted derivatives of the pyrimidine scaffold were also prepared via reaction of the N3-amino derivatives with a number of monosaccharides followed by acetylation.
RESULTS: The anticancer activity of the synthesized compounds was studied against human liver cancer (HepG2) and RPE-1cell lines. Compounds 2a, 2b, 3a and 12 showed potent activities with IC50 results comparable to that of doxorubicin.
CONCLUSION: Docking investigations into Cyclin-dependent kinase 2 (CDK-2) enzyme, a potential target for cancer medication, were also reported showing the possible binding interaction into the enzyme active site to support their activity behavior. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.

Entities:  

Keywords:  CDK2; Docking; HepG2; Pyrimidine; anticancer; glycosides; thiazolopyrimidine; thiopyrimidine.

Mesh：

Substances：

Year:  2019        PMID： 30864522     DOI： 10.2174/1389557519666190312165717

Source DB:  PubMed          Journal:  Mini Rev Med Chem        ISSN： 1389-5575            Impact factor:   3.862


  5 in total

1.  Novel 1,2,3-Triazole-Coumarin Hybrid Glycosides and Their Tetrazolyl Analogues: Design, Anticancer Evaluation and Molecular Docking Targeting EGFR, VEGFR-2 and CDK-2.

Authors:  Wael A El-Sayed; Fahad M Alminderej; Marwa M Mounier; Eman S Nossier; Sayed M Saleh; Asmaa F Kassem
Journal:  Molecules       Date:  2022-03-22       Impact factor: 4.411

2.  New 1,2,3-Triazole-Coumarin-Glycoside Hybrids and Their 1,2,4-Triazolyl Thioglycoside Analogs Targeting Mitochondria Apoptotic Pathway: Synthesis, Anticancer Activity and Docking Simulation.

Authors:  Wael A El-Sayed; Fahad M Alminderej; Marwa M Mounier; Eman S Nossier; Sayed M Saleh; Asmaa F Kassem
Journal:  Molecules       Date:  2022-09-03       Impact factor: 4.927

3.  Synthesis and Cytotoxic Activity of New Thiazolopyrimidine Sugar Hydrazones and Their Derived Acyclic Nucleoside Analogues.

Authors:  Ebtesam A Basiony; Allam A Hassan; Zahra M Al-Amshany; Ahmed A Abd-Rabou; Adel A-H Abdel-Rahman; Nasser A Hassan; Wael A El-Sayed
Journal:  Molecules       Date:  2020-01-18       Impact factor: 4.411

4.  Discovery of New Pyrazolopyridine, Furopyridine, and Pyridine Derivatives as CDK2 Inhibitors: Design, Synthesis, Docking Studies, and Anti-Proliferative Activity.

Authors:  Adel A-H Abdel-Rahman; Amira K F Shaban; Ibrahim F Nassar; Dina S El-Kady; Nasser S M Ismail; Samy F Mahmoud; Hanem M Awad; Wael A El-Sayed
Journal:  Molecules       Date:  2021-06-26       Impact factor: 4.411

5.  Click chemistry based synthesis, cytotoxic activity and molecular docking of novel triazole-thienopyrimidine hybrid glycosides targeting EGFR.

Authors:  Reham R Khattab; Asma K Alshamari; Allam A Hassan; Hussein H Elganzory; Wael A El-Sayed; Hanem M Awad; Eman S Nossier; Nasser A Hassan
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051
  5 in total

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