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Synthesis and SAR of novel tricyclic quinoxalinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Bioorg Med Chem Lett. 2009 Aug 01; 19(15):4050-4.BM

Abstract

Based on screening hit 1, a series of tricyclic quinoxalinones have been designed and evaluated for inhibition of PARP-1. Substitutions at the 7- and 8-positions of the quinoxalinone ring led to a number of compounds with good enzymatic and cellular potency. The tricyclic quinoxalinone class is sensitive to modifications of both the amine substituent and the tricyclic core. The synthesis and structure-activity relationship studies are presented.

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Authors+Show Affiliations

Miyashiro J
Cancer Research, GPRD, Abbott Laboratories, 100 Abbott Park Rd., Abbott Park, IL 60064, USA. julie.miyashiro@abbott.com
Woods KW
No affiliation info available
Park CH
No affiliation info available
Liu X
No affiliation info available
Shi Y
No affiliation info available
Johnson EF
No affiliation info available
Bouska JJ
No affiliation info available
Olson AM
No affiliation info available
Luo Y
No affiliation info available
Fry EH
No affiliation info available
Giranda VL
No affiliation info available
Penning TD
No affiliation info available

MeSH

Antineoplastic AgentsApoptosisCell NucleusChemistry, PharmaceuticalDNA RepairDrug DesignDrug Screening Assays, AntitumorHumansKineticsModels, MolecularMolecular ConformationNiacinamidePoly(ADP-ribose) Polymerase InhibitorsQuinoxalinesStructure-Activity Relationship

Pub Type(s)

Journal Article

Language

eng

PubMed ID

19553114

Citation

Miyashiro, Julie, et al. "Synthesis and SAR of Novel Tricyclic Quinoxalinone Inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1)." Bioorganic & Medicinal Chemistry Letters, vol. 19, no. 15, 2009, pp. 4050-4.
Miyashiro J, Woods KW, Park CH, et al. Synthesis and SAR of novel tricyclic quinoxalinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1). Bioorg Med Chem Lett. 2009;19(15):4050-4.
Miyashiro, J., Woods, K. W., Park, C. H., Liu, X., Shi, Y., Johnson, E. F., Bouska, J. J., Olson, A. M., Luo, Y., Fry, E. H., Giranda, V. L., & Penning, T. D. (2009). Synthesis and SAR of novel tricyclic quinoxalinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1). Bioorganic & Medicinal Chemistry Letters, 19(15), 4050-4. https://doi.org/10.1016/j.bmcl.2009.06.016
Miyashiro J, et al. Synthesis and SAR of Novel Tricyclic Quinoxalinone Inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1). Bioorg Med Chem Lett. 2009 Aug 1;19(15):4050-4. PubMed PMID: 19553114.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and SAR of novel tricyclic quinoxalinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1). AU - Miyashiro,Julie, AU - Woods,Keith W, AU - Park,Chang H, AU - Liu,Xuesong, AU - Shi,Yan, AU - Johnson,Eric F, AU - Bouska,Jennifer J, AU - Olson,Amanda M, AU - Luo,Yan, AU - Fry,Elizabeth H, AU - Giranda,Vincent L, AU - Penning,Thomas D, Y1 - 2009/06/13/ PY - 2009/04/21/received PY - 2009/06/03/revised PY - 2009/06/05/accepted PY - 2009/6/26/entrez PY - 2009/6/26/pubmed PY - 2009/12/16/medline SP - 4050 EP - 4 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 19 IS - 15 N2 - Based on screening hit 1, a series of tricyclic quinoxalinones have been designed and evaluated for inhibition of PARP-1. Substitutions at the 7- and 8-positions of the quinoxalinone ring led to a number of compounds with good enzymatic and cellular potency. The tricyclic quinoxalinone class is sensitive to modifications of both the amine substituent and the tricyclic core. The synthesis and structure-activity relationship studies are presented. SN - 1464-3405 UR - https://www.unboundmedicine.com/medline/citation/19553114/Synthesis_and_SAR_of_novel_tricyclic_quinoxalinone_inhibitors_of_poly_ADP_ribose_polymerase_1__PARP_1__ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(09)00848-8 DB - PRIME DP - Unbound Medicine ER -