| Literature DB >> 19700321 |
Christopher J Helal1, Zhijun Kang, John C Lucas, Thomas Gant, Michael K Ahlijanian, Joel B Schachter, Karl E G Richter, James M Cook, Frank S Menniti, Kristin Kelly, Scot Mente, Jay Pandit, Natalie Hosea.
Abstract
Utilizing structure-based drug design, a 4-aminoimidazole heterocyclic core was synthesized as a replacement for a 2-aminothiazole due to potential metabolically mediated toxicity. The synthetic route utilized allowed for ready synthesis of 1-substituted-4-aminoimidazoles. SAR exploration resulted in the identification of a novel cis-substituted cyclobutyl group that gave improved enzyme and cellular potency against cdk5/p25 with up to 30-fold selectivity over cdk2/cyclin E.Entities:
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Year: 2009 PMID： 19700321 DOI： 10.1016/j.bmcl.2009.08.019
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823