C. Kunick Pages 181 - 194 ( 14 )
Based on the observation that some simple [l]benzazepin-2-ones exhibit in vivo antitumor activity, studies directed to several new structure classes with this partial motif have been reported recently, comprising 7,l 2-dihydro-indolo[3,2-d][l ]benzazepin- 6(5H)-ones (paullones), 5H-quinolino[3,2-d][ I ]benzazepin-6(7H)-ones, 2,4-diaryl-5H• pyrido[3,2-d][ I ]benzazepin-6(7H)-ones, spiro[ l-benzazepine-4, l '-cyclohexane] deri va tives, and naphthannelated benzazepinones. For the syntheses of these heterocyclic compounds, IH-[l]benzazepine-2,5(3H,4H)-diones were employed as readily available ; starting materials. In each of the mentioned series, entities with in vitro antitumor activity have been detected. Considering potency and in vitro cell line selectivity, both the 2,4-diaryl-5H-pyrido[3,2-d][ I ]benzazepin- 6(7H)-ones and the paullones are apparently suitable for a further development. A biological mechanism probably related to the antiproliferative activity has been established only for the paullones. These compounds represent a novel class of selective inhibitors of cyclin-dependent kinases, a family of enzymes whose function seems to be deregulated in many human tumors.