期刊
CURRENT PHARMACEUTICAL DESIGN
卷 18, 期 20, 页码 2974-2980出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/138161212800672804
关键词
Cancer; cyclin-dependent kinase; inhibitor; roscovitine; bioisostere
资金
- Ministry of Education, Youth and Sports of the Czech Republic [MSM6198959216]
- Czech Science Foundation [P305/12/0783]
- European Regional Development Fund under grant FNUSA-ICRC [CZ.1.05/1.1.00/02.0123]
- EU under Marie Curie International Reintegration Grant [230936]
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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