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Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2 |
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| Authors: | Williamson Douglas S Parratt Martin J Bower Justin F Moore Jonathan D Richardson Christine M Dokurno Pawel Cansfield Andrew D Francis Geraint L Hebdon Richard J Howes Rob Jackson Philip S Lockie Andrea M Murray James B Nunns Claire L Powles Jenifer Robertson Alan Surgenor Allan E Torrance Christopher J |
| Affiliation: | Vernalis (R&D) Ltd, Granta Park, Great Abington, Cambridge CB1 6GB, United Kingdom. d.williamson@vernalis.com |
| 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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