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)
Current Topics in Medicinal Chemistry
Title: Paullones as Inhibitors of Protein Kinases
Volume: 11 Issue: 11
Author(s): Nadine Tolle and Conrad Kunick
Affiliation:
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)
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.
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Cite this article as:
Tolle Nadine and Kunick Conrad, Paullones as Inhibitors of Protein Kinases, Current Topics in Medicinal Chemistry 2011; 11 (11) . https://dx.doi.org/10.2174/156802611795589601
DOI https://dx.doi.org/10.2174/156802611795589601 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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