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ID: ALA1138164
Journal: Bioorg Med Chem Lett
Title: Synthesis and structure-activity relationships of novel pyrrolocarbazole lactam analogs as potent and cell-permeable inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Authors: Wells GJ, Bihovsky R, Hudkins RL, Ator MA, Husten J.
Abstract: A series of novel pyrrolocarbazole lactams was identified as potent PARP-1 inhibitors in vitro and in a PC12 cellular NAD(+) depletion assay. The SAR trends of substituents at the 3-position, as well as the effect of blocking the indole or lactam NH-groups of the template by methylation or formylation, are discussed in relation to molecular modeling studies.
CiteXplore: 16359865