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Updated: Aug 14, 2026

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors
Ming Tao1, Chung Ho Park, Ron Bihovsky
1Cephalon, Inc., 145 Brandywine Parkway, West Chester, PA 19380-4245, USA. mtao@cephalon.com
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.
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