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ID: ALA1146950

Journal: Bioorg Med Chem Lett

Title: Matrix compare analysis discriminates subtle structural differences in a family of novel antiproliferative agents, diaryl-3-hydroxy-2,3,3a,10a-tetrahydrobenzo[b]cycylopenta[e]azepine-4,10(1H,5H)-diones.

Authors: Kunick C, Bleeker C, Prühs C, Totzke F, Schächtele C, Kubbutat MH, Link A.

Abstract: A diastereoselective synthesis of 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. The novel compounds exhibit antiproliferative activity in a panel of in vitro cultivated cancer cell lines. The bioinformatic tool COMPARE was able to discriminate between two closely related subgroups of the title compounds, namely 1,3- and 2,3-disubstituted derivatives.

CiteXplore: 16464582

DOI: 10.1016/j.bmcl.2006.01.071