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. 2005 Feb 15;15(4):863-7.
doi: 10.1016/j.bmcl.2004.12.073.

Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2

Douglas S Williamson  1 , Martin J Parratt, Justin F Bower, Jonathan D Moore, Christine M Richardson, Pawel Dokurno, Andrew D Cansfield, Geraint L Francis, Richard J Hebdon, Rob Howes, Philip S Jackson, Andrea M Lockie, James B Murray, Claire L Nunns, Jenifer Powles, Alan Robertson, Allan E Surgenor, Christopher J Torrance
Affiliations

Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2

Douglas S Williamson et al. Bioorg Med Chem Lett. .

Abstract

The protein structure guided design of a series of pyrazolo[1,5-a]pyrimidines with high potency for human cyclin-dependent kinase 2 (CDK2) is described. Some examples were shown to inhibit the growth of human colon tumour cells, were equipotent for CDK1 and were selective against GSK-3beta and other kinases.

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