| Literature DB >> 18502127 |
Christopher Lum1, Jeff Kahl, Linda Kessler, Jeff Kucharski, Jan Lundström, Stephen Miller, Hiroshi Nakanishi, Yazhong Pei, Kent Pryor, Edward Roberts, Lubomir Sebo, Robert Sullivan, Jan Urban, Zhijun Wang.
Abstract
The discovery of two classes of pyrimidine-based inhibitors of GSK-3 is described. Optimization of these series led to inhibitors with IC(50)<10nM and >100-fold selectivity over Aurora A kinase. A proposed binding mode of 21b is presented. One compound (33) of the pyrimidine series showed promising pharmacokinetic parameters.Entities:
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Year: 2008 PMID： 18502127 DOI： 10.1016/j.bmcl.2008.05.001
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823