2. Academic Validation
  3. Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors

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

  • Bioorg Med Chem Lett. 2006 Feb 15;16(4):938-42. doi: 10.1016/j.bmcl.2005.10.099.
Ming Tao 1,  Chung Ho Park,  Ron Bihovsky,  Gregory J Wells,  Jean Husten,  Mark A Ator,  Robert L Hudkins
Affiliations

Affiliation

  • 1 Cephalon, Inc., 145 Brandywine Parkway, West Chester, PA 19380-4245, USA. mtao@cephalon.com
PMID: 16290935 DOI: 10.1016/j.bmcl.2005.10.099
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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