Journal
ORGANIC LETTERS
Volume 8, Issue 24, Pages 5465-5468Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ol0620646
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- NIA NIH HHS [AG 10124] Funding Source: Medline
- NIGMS NIH HHS [1 R01 GM071695-01A1] Funding Source: Medline
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Cyclopentadienyl half-sandwich ruthenium complexes have been demonstrated to be promising scaffolds as protein kinase inhibitors. In order to rapidly identify derivatives which display modified pharmacological properties, we developed the synthesis of an organoruthenium compound bearing an N-succinimidyl ester at the cyclopentadienyl moiety. The quenching of this activated ester with a library of primary amines, followed by testing of the resulting amide library, led to the identification of organometallic Pim-1 and GSK-3 inhibitors with improved potencies and kinase selectivities.
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