Bioorganic & Medicinal Chemistry Letters 2000-03-20

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

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

Index: Bioorg. Med. Chem. Lett. 10(6) , 567-9, (2000)

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Abstract

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.