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Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Bioorg Med Chem Lett. 2010 Jan 15; 20(2):448-52.BM

Abstract

A novel hexahydrobenzonaphthyridinone PARP-1 pharmacophore is reported, subsequent SAR exploration around this scaffold led to selective PARP-1 inhibitors with low nanomolar enzyme potency, displaying good cellular activity and promising rat PK properties.

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Authors+Show Affiliations

Torrisi C
IRBM-Merck Research Laboratories Rome, Via Pontina km 30,600, Pomezia, 00040 Rome, Italy. caterina.torrisi@addexpharma.com
Bisbocci M
No affiliation info available
Ingenito R
No affiliation info available
Ontoria JM
No affiliation info available
Rowley M
No affiliation info available
Schultz-Fademrecht C
No affiliation info available
Toniatti C
No affiliation info available
Jones P
No affiliation info available

MeSH

AnimalsDrug DiscoveryEnzyme InhibitorsMicrosomes, LiverNaphthyridinesPoly(ADP-ribose) Polymerase InhibitorsPoly(ADP-ribose) PolymerasesRatsStructure-Activity Relationship

Pub Type(s)

Journal Article

Language

eng

PubMed ID

20015648

Citation

Torrisi, Caterina, et al. "Discovery and SAR of Novel, Potent and Selective Hexahydrobenzonaphthyridinone Inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1)." Bioorganic & Medicinal Chemistry Letters, vol. 20, no. 2, 2010, pp. 448-52.
Torrisi C, Bisbocci M, Ingenito R, et al. Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1). Bioorg Med Chem Lett. 2010;20(2):448-52.
Torrisi, C., Bisbocci, M., Ingenito, R., Ontoria, J. M., Rowley, M., Schultz-Fademrecht, C., Toniatti, C., & Jones, P. (2010). Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1). Bioorganic & Medicinal Chemistry Letters, 20(2), 448-52. https://doi.org/10.1016/j.bmcl.2009.12.002
Torrisi C, et al. Discovery and SAR of Novel, Potent and Selective Hexahydrobenzonaphthyridinone Inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1). Bioorg Med Chem Lett. 2010 Jan 15;20(2):448-52. PubMed PMID: 20015648.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1). AU - Torrisi,Caterina, AU - Bisbocci,Monica, AU - Ingenito,Raffaele, AU - Ontoria,Jesus M, AU - Rowley,Michael, AU - Schultz-Fademrecht,Carsten, AU - Toniatti,Carlo, AU - Jones,Philip, Y1 - 2009/12/04/ PY - 2009/11/09/received PY - 2009/12/01/revised PY - 2009/12/01/accepted PY - 2009/12/18/entrez PY - 2009/12/18/pubmed PY - 2010/4/21/medline SP - 448 EP - 52 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 20 IS - 2 N2 - A novel hexahydrobenzonaphthyridinone PARP-1 pharmacophore is reported, subsequent SAR exploration around this scaffold led to selective PARP-1 inhibitors with low nanomolar enzyme potency, displaying good cellular activity and promising rat PK properties. SN - 1464-3405 UR - https://www.unboundmedicine.com/medline/citation/20015648/Discovery_and_SAR_of_novel_potent_and_selective_hexahydrobenzonaphthyridinone_inhibitors_of_poly_ADP_ribose_polymerase_1__PARP_1__ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(09)01703-X DB - PRIME DP - Unbound Medicine ER -