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

Author(s): Adel A.H. Abdel Rahman, Ibrahim F. Nassar*, Amira K.F. Shaban, Dina S. EL-Kady, Hanem M. Awad, Wael A. El Sayed*.

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 19 , Issue 13 , 2019

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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.

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VOLUME: 19
ISSUE: 13
Year: 2019
Page: [1093 - 1110]
Pages: 18
DOI: 10.2174/1389557519666190312165717
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