Design, synthesis, and biological evaluation of novel pyrimidine derivatives as CDK2 inhibitors.

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Ibrahim DA, El-Metwally AM

Design, synthesis, and biological evaluation of novel pyrimidine derivatives as CDK2 inhibitors.

Eur J Med Chem. 2010 Mar;45(3):1158-66. doi: 10.1016/j.ejmech.2009.12.026. Epub 2009 Dec 21.

PubMed ID

20045222 [ View in PubMed

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Abstract

Novel derivatives of 2,4,5,6-tetrasubstituted pyrimidine cyclin-dependent kinase (CDK2) inhibitors was designed and synthesized. We built a library of proposed pyrimidine derivatives and by using pharmacophore and docking techniques we made our selections. We modified the proposed compounds due to the interaction of docked structures with the protein to achieve the best fit. The newly synthesized compounds showed potent and selective CDK2 inhibitory activities and inhibited in-vitro cellular proliferation in cultured human tumor cells. The design, synthesis and biological evaluation of these 2,4,5,6-tetrasubstituted pyrimidine derivatives are reported.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Olomoucine	Cyclin-dependent kinase 2	IC 50 (nM)	7000	N/A	N/A	Details