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Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR |
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| Authors: | Richardson Christine M Williamson Douglas S Parratt Martin J Borgognoni Jenifer Cansfield Andrew D Dokurno Pawel Francis Geraint L Howes Rob Moore Jonathan D Murray James B Robertson Alan Surgenor Allan E Torrance Christopher J |
| Affiliation: | Vernalis (R&D) Ltd, Granta Park, Great Abington, Cambridge CB1 6GB, UK. |
| Abstract: | Crystallographic and modelling data, in conjunction with a medicinal chemistry template-hopping approach, led to the identification of a series of novel and potent inhibitors of human cyclin-dependent kinase 2 (CDK2), with selectivity over glycogen synthase kinase-3beta (GSK-3beta). One example had a CDK2 IC(50) of 120 nM and showed selectivity over GSK-3beta of 167-fold. |
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