Epoxide-containing side chains enhance antiproliferative activity of paullones
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Eur. J. Med. Chem. 2005, 40, 655-661.

Xu Xiea, Thomas Lemckea, Rick Gussiob, Daniel W. Zaharevitzb, Maryse Leostc, Laurent Meijerc and Conrad Kunickd

aInstitut für Pharmazie, Universität Hamburg, Bundesstraße 45, D-20146 Hamburg, Germany
bNational Cancer Institute, Executive Plaza North, Rockville, MD 20893, USA
cCentre National de la Recherche Scientifique, Station Biologique, BP 74, F-29682 Roscoff, France
dInstitut für Pharmazeutische Chemie, Technische Universität Braunschweig, Beethovenstraße 55, D-38106 Braunschweig, Germany

The introduction of side chains bearing epoxide motifs into the molecular scaffold of kenpaullone and 9-trifluoromethylpaullone led to improved antiproliferative activity of the novel derivatives for human tumor cell lines. The syntheses were accomplished applying Stille coupling for the introduction of unsaturated side chains into the 2-position of the paullones and subsequently employing a hydrogen peroxide/nitrile mixture for the epoxidation of C,C-double bonds.

Keywords: Antiproliferative activity; Cyclin-dependent kinases; Epoxides; Paullones; Stille coupling

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