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Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors.
Bioorg Med Chem Lett. 2008 Sep 15; 18(18):5126-9.BM

Abstract

A novel class of PARP-1 inhibitors was identified containing a non-aromatic heterocycle or carbocycle fused to a pyrazolo pyridin-2-one. Compounds displayed low nanomolar binding activity in the PARP-1 binding assay and submicromolar activity in a cell based chemosensitization assay.

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Authors+Show Affiliations

Moree WJ
Deltagen Research Laboratories (Former CombiChem, Inc.), 4570 Executive Drive, Suite 400, San Diego, CA 92121, USA. wmoree@neurocrine.com
Goldman P
No affiliation info available
Demaggio AJ
No affiliation info available
Christenson E
No affiliation info available
Herendeen D
No affiliation info available
Eksterowicz J
No affiliation info available
Kesicki EA
No affiliation info available
McElligott DL
No affiliation info available
Beaton G
No affiliation info available

MeSH

AnimalsChickensCombinatorial Chemistry TechniquesDrug DesignEnzyme InhibitorsMolecular StructurePoly(ADP-ribose) Polymerase InhibitorsPyrazolesPyridonesStructure-Activity Relationship

Pub Type(s)

Journal Article

Language

eng

PubMed ID

18713665

Citation

Moree, Wilna J., et al. "Identification of Ring-fused Pyrazolo Pyridin-2-ones as Novel poly(ADP-ribose)polymerase-1 Inhibitors." Bioorganic & Medicinal Chemistry Letters, vol. 18, no. 18, 2008, pp. 5126-9.
Moree WJ, Goldman P, Demaggio AJ, et al. Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors. Bioorg Med Chem Lett. 2008;18(18):5126-9.
Moree, W. J., Goldman, P., Demaggio, A. J., Christenson, E., Herendeen, D., Eksterowicz, J., Kesicki, E. A., McElligott, D. L., & Beaton, G. (2008). Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors. Bioorganic & Medicinal Chemistry Letters, 18(18), 5126-9. https://doi.org/10.1016/j.bmcl.2008.07.091
Moree WJ, et al. Identification of Ring-fused Pyrazolo Pyridin-2-ones as Novel poly(ADP-ribose)polymerase-1 Inhibitors. Bioorg Med Chem Lett. 2008 Sep 15;18(18):5126-9. PubMed PMID: 18713665.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors. AU - Moree,Wilna J, AU - Goldman,Phyllis, AU - Demaggio,Anthony J, AU - Christenson,Erik, AU - Herendeen,Dan, AU - Eksterowicz,John, AU - Kesicki,Edward A, AU - McElligott,David L, AU - Beaton,Graham, Y1 - 2008/07/27/ PY - 2008/05/27/received PY - 2008/07/23/revised PY - 2008/07/24/accepted PY - 2008/8/21/pubmed PY - 2008/10/15/medline PY - 2008/8/21/entrez SP - 5126 EP - 9 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 18 IS - 18 N2 - A novel class of PARP-1 inhibitors was identified containing a non-aromatic heterocycle or carbocycle fused to a pyrazolo pyridin-2-one. Compounds displayed low nanomolar binding activity in the PARP-1 binding assay and submicromolar activity in a cell based chemosensitization assay. SN - 1464-3405 UR - https://www.unboundmedicine.com/medline/citation/18713665/Identification_of_ring_fused_pyrazolo_pyridin_2_ones_as_novel_poly_ADP_ribose_polymerase_1_inhibitors_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(08)00871-8 DB - PRIME DP - Unbound Medicine ER -