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- Title
Cyclin-dependent kinase inhibitors inspired by roscovitine: purine bioisosteres.
- Authors
Jorda, Radek; Paruch, Kamil; Krystof, Vladimír
- Abstract
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.
- Publication
Current pharmaceutical design, 2012, Vol 18, Issue 20, p2974
- ISSN
1873-4286
- Publication type
Journal Article
- DOI
10.2174/138161212800672804