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.