Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones.
نویسندگان
چکیده
A remarkably concise, chromatography-free route to the parent compound of the paullone family of cyclin-dependent kinase (CDK) inhibitors is reported. A similar strategy allowed the synthesis of the hitherto missing 9-azapaullone and its protonated, N-oxidised and N-alkylated derivatives. Screening studies identified an active and strongly selective inhibitor of CDK9/cyclin T.
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ورودعنوان ژورنال:
- Bioorganic & medicinal chemistry letters
دوره 20 16 شماره
صفحات -
تاریخ انتشار 2010