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