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Discovery of thiophene inhibitors of polo-like kinase.
Identification of GSK461364, a novel small molecule polo-like kinase 1 inhibitor for the treatment of cancer
This presentation will highlight the lead optimization studies and elucidation of the structure-activity relationship leading to the identification of a novel thiophene amide Plk1 inhibitor, with greater than 100-fold selectivity across a panel of 47 other kinases.
Free Radical-Mediated Vinyl Amination: Access to N,N-Dialkyl Enamines and Their β-Stannyl and β-Thio Derivatives
The first examples of free radical-mediated vinyl amination are described by nonconventional vinyl radical addition to azomethine nitrogen. This new vinyl amination protocol is mild and provides
Free radical-mediated vinyl amination: access to N,N-dialkyl enamines and their beta-stannyl and beta-thio derivatives.
This new vinyl amination protocol is mild and provides convenient synthetic access to nonstabilized N,N-dialkyl enamines and tandem bond-forming processes.