2. Academic Validation
  3. 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

  • 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

Affiliation

  • 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.

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