Kunick et al.16 synthesized diastereoselective diaryl-3-hydroxy-2,3,3a,10a-tetrahydrobenzo[b]cycylopenta[e]azepine-4,10(1H,5H)-diones is described employing a tandem Michael-aldol addition as key step (Scheme 1). The novel compounds exhibit antiproliferative activity in a panel of in vitro cultivated cancer cell lines.
16. C. Kunick, C. Bleeker, C. Prühs, C. S. Totzke, M. H. J. Kubbutat, and A. Link, Bioorg. Med. Chem. Lett., 2006, 16, 2148.
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