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Identification of substituted pyrazolo[1,5-a]quinazolin-5(4H)-one as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors.
Bioorg Med Chem Lett. 2009 Aug 01; 19(15):4196-200.BM

Abstract

A novel series of pyrazolo[1,5-a]quinazolin-5(4H)-one derivatives proved to be a potent class of PARP-1 inhibitors. An extensive SAR around the 3-position of pyrazole in the scaffold led to the discovery of amides derivatives as low nanomolar PARP-1 inhibitors.

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Authors+Show Affiliations

Orvieto F
IRBM - Merck Research Laboratories Rome, Via Pontina km 30,600, Pomezia, 00040 Rome, Italy. federica_orvieto@merck.com
Branca D
No affiliation info available
Giomini C
No affiliation info available
Jones P
No affiliation info available
Koch U
No affiliation info available
Ontoria JM
No affiliation info available
Palumbi MC
No affiliation info available
Rowley M
No affiliation info available
Toniatti C
No affiliation info available
Muraglia E
No affiliation info available

MeSH

AmidesChemistry, OrganicChemistry, PharmaceuticalDrug DesignDrug Evaluation, PreclinicalEnzyme InhibitorsHeLa CellsHumansInhibitory Concentration 50Models, ChemicalMolecular StructurePoly(ADP-ribose) Polymerase InhibitorsPyrazolesQuinazolinonesStructure-Activity Relationship

Pub Type(s)

Journal Article

Language

eng

PubMed ID

19541484

Citation

Orvieto, Federica, et al. "Identification of Substituted pyrazolo[1,5-a]quinazolin-5(4H)-one as Potent poly(ADP-ribose)polymerase-1 (PARP-1) Inhibitors." Bioorganic & Medicinal Chemistry Letters, vol. 19, no. 15, 2009, pp. 4196-200.
Orvieto F, Branca D, Giomini C, et al. Identification of substituted pyrazolo[1,5-a]quinazolin-5(4H)-one as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors. Bioorg Med Chem Lett. 2009;19(15):4196-200.
Orvieto, F., Branca, D., Giomini, C., Jones, P., Koch, U., Ontoria, J. M., Palumbi, M. C., Rowley, M., Toniatti, C., & Muraglia, E. (2009). Identification of substituted pyrazolo[1,5-a]quinazolin-5(4H)-one as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors. Bioorganic & Medicinal Chemistry Letters, 19(15), 4196-200. https://doi.org/10.1016/j.bmcl.2009.05.113
Orvieto F, et al. Identification of Substituted pyrazolo[1,5-a]quinazolin-5(4H)-one as Potent poly(ADP-ribose)polymerase-1 (PARP-1) Inhibitors. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4196-200. PubMed PMID: 19541484.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Identification of substituted pyrazolo[1,5-a]quinazolin-5(4H)-one as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors. AU - Orvieto,Federica, AU - Branca,Danila, AU - Giomini,Claudia, AU - Jones,Philip, AU - Koch,Uwe, AU - Ontoria,Jesus M, AU - Palumbi,Maria Cecilia, AU - Rowley,Michael, AU - Toniatti,Carlo, AU - Muraglia,Ester, Y1 - 2009/06/02/ PY - 2009/04/29/received PY - 2009/05/27/revised PY - 2009/05/27/accepted PY - 2009/6/23/entrez PY - 2009/6/23/pubmed PY - 2009/12/16/medline SP - 4196 EP - 200 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 19 IS - 15 N2 - A novel series of pyrazolo[1,5-a]quinazolin-5(4H)-one derivatives proved to be a potent class of PARP-1 inhibitors. An extensive SAR around the 3-position of pyrazole in the scaffold led to the discovery of amides derivatives as low nanomolar PARP-1 inhibitors. SN - 1464-3405 UR - https://www.unboundmedicine.com/medline/citation/19541484/Identification_of_substituted_pyrazolo[15_a]quinazolin_5_4H__one_as_potent_poly_ADP_ribose_polymerase_1__PARP_1__inhibitors_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(09)00818-X DB - PRIME DP - Unbound Medicine ER -