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.
As analogues to the paullone kinase inhibitor family, boron chelate complexes of 4-anilinomethylidene-1-benzazepine-2,5-diones were prepared by reacting the ligands with boron trifluoride etherate or triphenylborane. The structures of the novel heterocyclic ring systems were established by X-ray structure analysis of two representative derivatives. The stability of the compounds in dimethylsulfoxide solution is dependent on the electronic properties of the aryl ring substituents. The fluorescent properties of the molecules are suitable for imaging the intracellular compound distribution by confocal laser microscopy.
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