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

  • Bioorg Med Chem Lett. 2000 Mar 20;10(6):567-9. doi: 10.1016/s0960-894x(00)00048-2.
C Kunick  1 ,  C Schultz ,  T Lemcke ,  D W Zaharevitz ,  R Gussio ,  R K Jalluri ,  E A Sausville ,  M Leost ,  L Meijer
Affiliations
  • 1. Institut für Pharmazie, Abteilung für Pharmazeutische Chemie, Universität Hamburg, Germany. [email protected]
PMID: 10741555 DOI: 10.1016/s0960-894x(00)00048-2
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.