Synthesis and biological evaluation of bengacarboline derivatives

Bengacarboline derivatives ( 11– 13 and 15) were synthesized. Seco derivatives 11 and 12 display a cytotoxic activity by inducing an accumulation of cells in the S phase of DNA synthesis Novel derivatives of the marine alkaloid bengacarboline have been synthesized. The seco derivatives 11 and 12 wer...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2008-02, Vol.18 (3), p.1212-1216
Hauptverfasser: Pouilhès, Annie, Kouklovsky, Cyrille, Langlois, Yves, Baltaze, Jean-Pierre, Vispé, Stéphane, Annereau, Jean-Philippe, Barret, Jean-Marc, Kruczynski, Anna, Bailly, Christian
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Sprache:eng
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Zusammenfassung:Bengacarboline derivatives ( 11– 13 and 15) were synthesized. Seco derivatives 11 and 12 display a cytotoxic activity by inducing an accumulation of cells in the S phase of DNA synthesis Novel derivatives of the marine alkaloid bengacarboline have been synthesized. The seco derivatives 11 and 12 were evaluated for topoisomerase inhibition, DNA damages, cytotoxicity and cell cycle perturbation. The two synthetic analogs are more potent cytotoxic agents than bengacarboline and they both induce an accumulation of cells in the S phase of DNA synthesis. They do not function as topoisomerase inhibitors but trigger DNA damages in cells.
ISSN:0960-894X
0968-0896
1464-3405
1464-3391
DOI:10.1016/j.bmcl.2007.11.113