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Synthesis and structure-activity relationships of novel pyrrolocarbazole lactam analogs as potent and cell-permeable inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Bioorg Med Chem Lett. 2006 Mar 01; 16(5):1151-5.BM

Abstract

A series of novel pyrrolocarbazole lactams was identified as potent PARP-1 inhibitors in vitro and in a PC12 cellular NAD(+) depletion assay. The SAR trends of substituents at the 3-position, as well as the effect of blocking the indole or lactam NH-groups of the template by methylation or formylation, are discussed in relation to molecular modeling studies.

Authors+Show Affiliations

Wells GJ
Cephalon, Inc., 145 Brandywine Parkway, West Chester, PA 19380-4245, USA. gwells@cephalon.com
Bihovsky R
No affiliation info available
Hudkins RL
No affiliation info available
Ator MA
No affiliation info available
Husten J
No affiliation info available

MeSH

AnimalsCarbazolesCell Membrane PermeabilityEnzyme InhibitorsImidesInhibitory Concentration 50LactamsModels, MolecularPC12 CellsPoly(ADP-ribose) Polymerase InhibitorsPoly(ADP-ribose) PolymerasesProtein Structure, TertiaryPyrrolesRatsStructure-Activity Relationship

Pub Type(s)

Journal Article

Language

eng

PubMed ID

16359865

Citation

Wells, Gregory J., et al. "Synthesis and Structure-activity Relationships of Novel Pyrrolocarbazole Lactam Analogs as Potent and Cell-permeable Inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1)." Bioorganic & Medicinal Chemistry Letters, vol. 16, no. 5, 2006, pp. 1151-5.
Wells GJ, Bihovsky R, Hudkins RL, et al. Synthesis and structure-activity relationships of novel pyrrolocarbazole lactam analogs as potent and cell-permeable inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1). Bioorg Med Chem Lett. 2006;16(5):1151-5.
Wells, G. J., Bihovsky, R., Hudkins, R. L., Ator, M. A., & Husten, J. (2006). Synthesis and structure-activity relationships of novel pyrrolocarbazole lactam analogs as potent and cell-permeable inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1). Bioorganic & Medicinal Chemistry Letters, 16(5), 1151-5.
Wells GJ, et al. Synthesis and Structure-activity Relationships of Novel Pyrrolocarbazole Lactam Analogs as Potent and Cell-permeable Inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1). Bioorg Med Chem Lett. 2006 Mar 1;16(5):1151-5. PubMed PMID: 16359865.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and structure-activity relationships of novel pyrrolocarbazole lactam analogs as potent and cell-permeable inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1). AU - Wells,Gregory J, AU - Bihovsky,Ron, AU - Hudkins,Robert L, AU - Ator,Mark A, AU - Husten,Jean, Y1 - 2005/12/15/ PY - 2005/10/05/received PY - 2005/11/24/revised PY - 2005/11/28/accepted PY - 2005/12/20/pubmed PY - 2006/3/24/medline PY - 2005/12/20/entrez SP - 1151 EP - 5 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 16 IS - 5 N2 - A series of novel pyrrolocarbazole lactams was identified as potent PARP-1 inhibitors in vitro and in a PC12 cellular NAD(+) depletion assay. The SAR trends of substituents at the 3-position, as well as the effect of blocking the indole or lactam NH-groups of the template by methylation or formylation, are discussed in relation to molecular modeling studies. SN - 0960-894X UR - https://www.unboundmedicine.com/medline/citation/16359865/Synthesis_and_structure_activity_relationships_of_novel_pyrrolocarbazole_lactam_analogs_as_potent_and_cell_permeable_inhibitors_of_poly_ADP_ribose_polymerase_1__PARP_1__ DB - PRIME DP - Unbound Medicine ER -