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

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

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

Bioorg Med Chem Lett. 2006 Feb 15;16(4):938-42. Epub 2005 Nov 15.

PubMed ID

16290935 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
6-AMINO-BENZO[DE]ISOQUINOLINE-1,3-DIONE	Poly [ADP-ribose] polymerase 1	IC 50 (nM)	26	N/A	N/A	Details