Document Detail

Cyclin-dependent kinase Inhibitors Inspired by Roscovitine: Purine Bioisosteres.
MedLine Citation:
PMID:  22571665     Owner:  NLM     Status:  Publisher    
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-α]-1,3,5-triazines, pyrazolo[1,5 α]pyrimidines, pyrazolo[1,5 α]pyridines and pyrazolo[4,3 d]pyrimidines.
Radek Jorda; Kamil Paruch; Vladimír Kryštof
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-5-7
Journal Detail:
Title:  Current pharmaceutical design     Volume:  -     ISSN:  1873-4286     ISO Abbreviation:  -     Publication Date:  2012 May 
Date Detail:
Created Date:  2012-5-10     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9602487     Medline TA:  Curr Pharm Des     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Laboratory of Growth Regulators, Palacký University, Šlechtitelů 11, 78371, Olomouc, Czech Republic.
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