4.4 Review

Paullones as Inhibitors of Protein Kinases

Journal

CURRENT TOPICS IN MEDICINAL CHEMISTRY
Volume 11, Issue 11, Pages 1320-1332

Publisher

BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/156802611795589601

Keywords

Azepinones; cyclin dependent kinases; GSK-3; indoles; paullones

Funding

  1. European Commission [LSHB-CT-2004-503467]

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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.

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