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

[ Vol. 19 , Issue. 13 ]

Author(s):

Adel A. H. Abdel Rahman, Ibrahim F. Nassar*, Amira K. F. Shaban, Dina S. EL-Kady, Hanem M. Awad and Wael A. El Sayed   Pages 1093 - 1110 ( 18 )

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.

Keywords:

Pyrimidine, thiopyrimidine, thiazolopyrimidine, glycosides, anticancer, HepG2, Docking, CDK2.

Affiliation:

Chemistry Department, Faculty of Science, Menofia University, Shebin El-Kom, Faculty of Specific Education, Ain Shams University, Abassia, Cairo, Chemistry Department, Faculty of Science, Menofia University, Shebin El-Kom, Hormone Department, National Research Centre, Dokki, Cairo, Tanning Materials and Leather Technology Department, National Research Centre, Dokki, Cairo, Chemistry Department, Faculty of Science, Qassim University



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