Tags

Type your tag names separated by a space and hit enter

Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors.
Bioorg Med Chem Lett. 2006 Feb 15; 16(4):938-42.BM

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.

Authors+Show Affiliations

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

MeSH

CarbazolesCrystallography, X-RayEnzyme InhibitorsHumansModels, MolecularMolecular StructurePoly (ADP-Ribose) Polymerase-1Poly(ADP-ribose) Polymerase InhibitorsStructure-Activity Relationship

Pub Type(s)

Journal Article

Language

eng

PubMed ID

16290935

Citation

Tao, Ming, et al. "Synthesis and Structure-activity Relationships of Novel poly(ADP-ribose) Polymerase-1 Inhibitors." Bioorganic & Medicinal Chemistry Letters, vol. 16, no. 4, 2006, pp. 938-42.
Tao M, Park CH, Bihovsky R, et al. Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors. Bioorg Med Chem Lett. 2006;16(4):938-42.
Tao, M., Park, C. H., Bihovsky, R., Wells, G. J., Husten, J., Ator, M. A., & Hudkins, R. L. (2006). Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors. Bioorganic & Medicinal Chemistry Letters, 16(4), 938-42.
Tao M, et al. Synthesis and Structure-activity Relationships of Novel poly(ADP-ribose) Polymerase-1 Inhibitors. Bioorg Med Chem Lett. 2006 Feb 15;16(4):938-42. PubMed PMID: 16290935.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors. AU - Tao,Ming, AU - Park,Chung Ho, AU - Bihovsky,Ron, AU - Wells,Gregory J, AU - Husten,Jean, AU - Ator,Mark A, AU - Hudkins,Robert L, Y1 - 2005/11/15/ PY - 2005/09/19/received PY - 2005/10/26/revised PY - 2005/10/28/accepted PY - 2005/11/18/pubmed PY - 2006/4/28/medline PY - 2005/11/18/entrez SP - 938 EP - 42 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 16 IS - 4 N2 - 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. SN - 0960-894X UR - https://www.unboundmedicine.com/medline/citation/16290935/Synthesis_and_structure_activity_relationships_of_novel_poly_ADP_ribose__polymerase_1_inhibitors_ DB - PRIME DP - Unbound Medicine ER -