Synthesis and structure-activity relationships of novel pyrrolocarbazole lactam analogs as potent and cell-permeable inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
作者： Gregory J. Wells , Ron Bihovsky , Robert L. Hudkins , Mark A. Ator , Jean Husten
DOI: 10.1016/J.BMCL.2005.11.086
关键词:
摘要: A series of novel pyrrolocarbazole lactams was identified as potent PARP-1 inhibitors in vitro and a PC12 cellular NAD + depletion assay. The SAR trends substituents at the 3-position, well effect blocking indole or lactam NH-groups template by methylation formylation, are discussed relation to molecular modeling studies.
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