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Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase.
Bioorg Med Chem Lett. 2008 Jul 15; 18(14):3942-5.BM

Abstract

We have previously described poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors based on a substituted benzyl-phthalazinone scaffold. As an alternative chemical template, a novel series of alkoxybenzamides were developed with restricted conformation through intramolecular hydrogen bond formation; the compounds exhibit low nM enzyme and cellular activity as PARP-1 inhibitors.

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Publisher Full Text (DOI)

Authors+Show Affiliations

Menear KA
KuDOS Pharmaceuticals Ltd, 410 Cambridge Science Park, Milton Road, Cambridge CB4 0PE, UK. kmenear@kudospharma.co.uk
Adcock C
No affiliation info available
Alonso FC
No affiliation info available
Blackburn K
No affiliation info available
Copsey L
No affiliation info available
Drzewiecki J
No affiliation info available
Fundo A
No affiliation info available
Le Gall A
No affiliation info available
Gomez S
No affiliation info available
Javaid H
No affiliation info available
Lence CF
No affiliation info available
Martin NM
No affiliation info available
Mydlowski C
No affiliation info available
Smith GC
No affiliation info available

MeSH

Chemistry, PharmaceuticalDrug DesignEnzyme InhibitorsHeLa CellsHumansHydrogen BondingInhibitory Concentration 50Models, ChemicalMolecular ConformationMolecular StructurePoly (ADP-Ribose) Polymerase-1Poly(ADP-ribose) Polymerase InhibitorsPoly(ADP-ribose) PolymerasesStructure-Activity RelationshipSubstrate Specificity

Pub Type(s)

Journal Article

Language

eng

PubMed ID

18579376

Citation

Menear, Keith A., et al. "Novel Alkoxybenzamide Inhibitors of poly(ADP-ribose) Polymerase." Bioorganic & Medicinal Chemistry Letters, vol. 18, no. 14, 2008, pp. 3942-5.
Menear KA, Adcock C, Alonso FC, et al. Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase. Bioorg Med Chem Lett. 2008;18(14):3942-5.
Menear, K. A., Adcock, C., Alonso, F. C., Blackburn, K., Copsey, L., Drzewiecki, J., Fundo, A., Le Gall, A., Gomez, S., Javaid, H., Lence, C. F., Martin, N. M., Mydlowski, C., & Smith, G. C. (2008). Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase. Bioorganic & Medicinal Chemistry Letters, 18(14), 3942-5. https://doi.org/10.1016/j.bmcl.2008.06.025
Menear KA, et al. Novel Alkoxybenzamide Inhibitors of poly(ADP-ribose) Polymerase. Bioorg Med Chem Lett. 2008 Jul 15;18(14):3942-5. PubMed PMID: 18579376.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase. AU - Menear,Keith A, AU - Adcock,Claire, AU - Alonso,Francisco Cuenca, AU - Blackburn,Kristel, AU - Copsey,Louise, AU - Drzewiecki,Jan, AU - Fundo,Alexandra, AU - Le Gall,Armelle, AU - Gomez,Sylvie, AU - Javaid,Hashim, AU - Lence,Carlos Fenandez, AU - Martin,Niall M B, AU - Mydlowski,Chris, AU - Smith,Graeme C M, Y1 - 2008/06/12/ PY - 2008/02/06/received PY - 2008/06/06/revised PY - 2008/06/06/accepted PY - 2008/6/27/pubmed PY - 2008/11/18/medline PY - 2008/6/27/entrez SP - 3942 EP - 5 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 18 IS - 14 N2 - We have previously described poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors based on a substituted benzyl-phthalazinone scaffold. As an alternative chemical template, a novel series of alkoxybenzamides were developed with restricted conformation through intramolecular hydrogen bond formation; the compounds exhibit low nM enzyme and cellular activity as PARP-1 inhibitors. SN - 1464-3405 UR - https://www.unboundmedicine.com/medline/citation/18579376/Novel_alkoxybenzamide_inhibitors_of_poly_ADP_ribose__polymerase_ DB - PRIME DP - Unbound Medicine ER -