2-Substituted paullones: CDK1/cyclin B-inhibiting property and in vitro antiproliferative activity.

2-Substituted paullones: CDK1/cyclin B-inhibiting property and in vitro antiproliferative activity.

Bioorganic & medicinal chemistry letters (2000-03-31)

C Kunick, C Schultz, T Lemcke, D W Zaharevitz, R Gussio, R K Jalluri, E A Sausville, M Leost, L Meijer

摘要

9-Trifluoromethyl-paullones with a carbon chain in the 2-position were synthesized by palladium-catalyzed coupling reactions of a 2-iodoprecursor with terminal alkenes or alkynes, respectively. The introduction of a 2-cyanoethyl substituent led to a significant enhancement of CDK1/cyclin B inhibiting property and in vitro antiproliferative activity.