Title of article
Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: Protein structure-guided design and SAR
Author/Authors
Christine M. Richardson، نويسنده , , Douglas S. Williamson، نويسنده , , Martin J. Parratt، نويسنده , , Jenifer Borgognoni، نويسنده , , Andrew D. Cansfield، نويسنده , , Pawel Dokurno، نويسنده , , Geraint L. Francis، نويسنده , , Rob Howes، نويسنده , , Jonathan D. Moore، نويسنده , , James B. Murray، نويسنده , , Alan Robertson، نويسنده , , Allan E. Surgenor، نويسنده , , Christopher J. Torrance، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
1353
To page
1357
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-3β (GSK-3β). One example had a CDK2 IC50 of 120 nM and showed selectivity over GSK-3β of 167-fold.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796577
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