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ID: ALA1148616

Journal: Bioorg Med Chem Lett

Title: Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors.

Authors: Tao M, Park CH, Bihovsky R, Wells GJ, Husten J, Ator MA, Hudkins RL.

Abstract: A series of novel pyrrolocarbazoles was synthesized as potential PARP-1 inhibitors. Pyrrolocarbazole 1 was identified as a potent PARP-1 inhibitor (IC50 = 36 nM) from our internal database. Synthesis of analogs around this template with the aid of modeling studies led to the identification of the truncated imide 14. Compound 14 (IC50 = 40 nM), with deleted B-ring, was found to be an equipotent PARP-1 inhibitor.

CiteXplore: 16290935

DOI: 10.1016/j.bmcl.2005.10.099