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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Paullones as Inhibitors of Protein Kinases

Author(s): Nadine Tolle and Conrad Kunick

Volume 11, Issue 11, 2011

Page: [1320 - 1332] Pages: 13

DOI: 10.2174/156802611795589601

Price: $65

Abstract

Paullones are a class of molecules structurally based on the 7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one parent scaffold. Many of these structures are inhibitors of certain protein kinases, namely cyclin-dependent kinases and glycogen synthase kinase-3. Being well referenced in the literature on the one hand and commercially available on the other hand, paullones have been used as biochemical tools in basic research and drug development for more than a decade. This review gives an overview over the published reports regarding chemistry, biological activity and pharmacological applications of paullone derivatives.

Keywords: Azepinones, cyclin dependent kinases, GSK-3, indoles, paullones, protein kinase inhibitors, cancer, glycogen synthase kinase-3, screening project, antiproliferative activity, COMPARE, chemotypes inhibiting cyclin-dependent kinases (CDKs)


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