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2-Substituted paullones: CDK1/cyclin B-inhibiting property and in vitro antiproliferative activity
Authors:Kunick C  Schultz C  Lemcke T  Zaharevitz D W  Gussio R  Jalluri R K  Sausville E A  Leost M  Meijer L
Affiliation:1. Center of Materials and Nanotechnologies, Faculty of Chemical Technology, University of Pardubice, Pardubice 532 10, Czech Republic;2. Department of General and Inorganic Chemistry, Faculty of Chemical Technology, University of Pardubice, Pardubice 532 10, Czech Republic;1. Institute of Physics and Technology, National Research Tomsk Polytechnic University, Tomsk, 634050, Russia;2. Institut für Physikalische und Theoretische Chemie, Technische Universität Braunschweig, D-38106, Braunschweig, Germany
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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