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

Synthesis, Docking Studies into CDK-2 and Anticancer Activity of New Derivatives Based Pyrimidine Scaffold and Their Derived Glycosides.
Mini Rev Med Chem. 2019 Mar 12;:
Authors: Rahman AAHA, Nassar IF, Shaban AKF, El-Kady DS, Awad HM, El Sayed WA
Abstract
New diaryl-substituted pyrimidinedione compounds, their thioxo derivatives as well as their bicyclic thiazole compounds were synthesized and characterized. 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. 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. 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.
PMID: 30864522 [PubMed - as supplied by publisher]

Source: Mini Reviews in Medicinal Chemistry - March 11, 2019 Category: Chemistry Authors: Rahman AAHA, Nassar IF, Shaban AKF, El-Kady DS, Awad HM, El Sayed WA Tags: Mini Rev Med Chem Source Type: research