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Cyclin-dependent kinase Inhibitors Inspired by Roscovitine: Purine Bioisosteres

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Roscovitine is a synthetic inhibitor of cyclin-dependent kinases that is currently undergoing clinical trials as a candidate drug for some oncological indications. Its discovery prompted many research teams to further optimize its structure or to initiate their own related but independent studies. This article reviews known roscovitine bioisosteres that have been prepared as CDK inhibitors using different core heterocycles. The individual bioisostere types have been described and explored to a different extent, which complicates direct comparisons of their biochemical activity - only six direct analogs containing different purine bioisosteres have been prepared and evaluated side by side with roscovitine. Only four types of bioisosteres have demonstrated improved biological properties, namely pyrazolo[ 1,5-a]-1,3,5-triazines, pyrazolo[1,5-a]pyrimidines, pyrazolo[1,5-a]pyridines and pyrazolo[4,3-d]pyrimidines.
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Keywords: CDK active site; Cancer; bioisostere; clinical trials; cyclin-dependent kinase; enantiomers; inhibitor; oncogenes; purine; roscovitine

Document Type: Research Article

Affiliations: Laboratory of Growth Regulators, Palacky University, Slechtitelu 11, 78371, Olomouc, Czech Republic.

Publication date: July 1, 2012

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    Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design, including: medicinal chemistry, pharmacology, drug targets and disease mechanism.
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