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8-Azapurines as new inhibitors of cyclin-dependent kinases.

Abstract：

:Purine inhibitors of cyclin-dependent kinases (CDK) seem to be a potential anticancer drug candidate as one of the first representatives, roscovitine, is passing Phase II clinical trials for cancer and glomerulonephritis. In this article, we describe a novel modification of the purine scaffold influencing CDK2 inhibitory activities as well as anticancer properties in cell lines of different histopathological origin. The introduced N at position 8 of the purine ring generally lowered CDK2 inhibitory activity of new 8-azapurines (1,2,3-triazolo[4,5-d]pyrimidines) in comparison to the model trisubstituted purines, whereas the antiproliferative potential of some derivatives remained very high, reflecting their ability to activate p53 tumor suppressor.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Havlicek L,Fuksova K,Krystof V,Orsag M,Vojtesek B,Strnad M

doi

10.1016/j.bmc.2005.06.007

subject

Has Abstract

pub_date

2005-09-15 00:00:00

pages

5399-407

issue

18

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(05)00513-4

journal_volume

13

pub_type

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