title: Serendipitous discovery of a prodrug of a PARP-1 inhibitor.
abstract: During SAR development of previously reported pyrrolocarbazole 1, a potent PARP-1 inhibitor, compound 14, was discovered serendipitously to be a prodrug of compound 1.
authors.affiliation: Cephalon, Inc., 145 Brandywine Parkway, West Chester, PA, 19380-4245, USA.
authors.forename: Derek
authors.initials: D
authors.lastname: Dunn
authors.forename: Jean
authors.initials: J
authors.lastname: Husten
authors.forename: Lisa D
authors.initials: LD
authors.lastname: Aimone
authors.forename: Mark A
authors.initials: MA
authors.lastname: Ator
authors.forename: Sankar
authors.initials: S
authors.lastname: Chatterjee
mesh_terms: D000818:Animals; D002227:Carbazoles / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics; D002645:Chickens; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics; D006207:Half-Life; D010797:Phthalimides / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics; D000067856:Poly(ADP-ribose) Polymerase Inhibitors; D011065:Poly(ADP-ribose) Polymerases / Q000378:metabolism; D011355:Prodrugs / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics; D011485:Protein Binding; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D002227:Carbazoles; D004791:Enzyme Inhibitors; D010797:Phthalimides; D000067856:Poly(ADP-ribose) Polymerase Inhibitors; D011355:Prodrugs; D011065:Poly(ADP-ribose) Polymerases
keywords: PARP-1; oncology; pyrrolocarbazole