Literature DB >> 19553114

Synthesis and SAR of novel tricyclic quinoxalinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).

Julie Miyashiro1, Keith W Woods, Chang H Park, Xuesong Liu, Yan Shi, Eric F Johnson, Jennifer J Bouska, Amanda M Olson, Yan Luo, Elizabeth H Fry, Vincent L Giranda, Thomas D Penning.   

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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Year:  2009        PMID: 19553114     DOI: 10.1016/j.bmcl.2009.06.016

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  18 in total

1.  Synthesis of Kappa Opioid Antagonists Based On Pyrrolo[1,2-α]quinoxalinones Using an N-Arylation/Condensation/Oxidation Reaction Sequence.

Authors:  Sarah M Scarry; Kimberly M Lovell; Kevin J Frankowski; Laura M Bohn; Jeffrey Aubé
Journal:  J Org Chem       Date:  2016-08-02       Impact factor: 4.354

2.  Concise route to a series of novel 3-(tetrazol-5-yl)quinoxalin-2(1H)-ones.

Authors:  Steven Gunawan; Gary Nichol; Christopher Hulme
Journal:  Tetrahedron Lett       Date:  2012-01-28       Impact factor: 2.415

3.  Nanoparticle-mediated measurement of target-drug binding in cancer cells.

Authors:  Adeeti V Ullal; Thomas Reiner; Katherine S Yang; Rostic Gorbatov; Changwook Min; David Issadore; Hakho Lee; Ralph Weissleder
Journal:  ACS Nano       Date:  2011-10-13       Impact factor: 15.881

4.  Synthesis of Pyrrolopyrazinones by Construction of the Pyrrole Ring onto an Intact Diketopiperazine.

Authors:  Susanna K Maisto; Angela P Leersnyder; Gwyneth L Pudner; Jonathan R Scheerer
Journal:  J Org Chem       Date:  2020-06-30       Impact factor: 4.354

5.  4-[(2,5-Dimethyl-anilino)acet-yl]-3,4-di-hydro-quinoxalin-2(1H)-one.

Authors:  Waqar Nasir; Munawar Ali Munawar; Saeed Ahmad; Sohail Nadeem; Muhammad Shahid
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-11-07

Review 6.  PARP-1 mechanism for coupling DNA damage detection to poly(ADP-ribose) synthesis.

Authors:  Marie-France Langelier; John M Pascal
Journal:  Curr Opin Struct Biol       Date:  2013-01-16       Impact factor: 6.809

7.  The LC Domain of hnRNPA2 Adopts Similar Conformations in Hydrogel Polymers, Liquid-like Droplets, and Nuclei.

Authors:  Siheng Xiang; Masato Kato; Leeju C Wu; Yi Lin; Ming Ding; Yajie Zhang; Yonghao Yu; Steven L McKnight
Journal:  Cell       Date:  2015-11-05       Impact factor: 41.582

8.  Active site fingerprinting and pharmacophore screening strategies for the identification of dual inhibitors of protein kinase C (ΡΚCβ) and poly (ADP-ribose) polymerase-1 (PARP-1).

Authors:  Navriti Chadha; Om Silakari
Journal:  Mol Divers       Date:  2016-05-23       Impact factor: 2.943

9.  Inhibition of poly(ADP-ribose) polymerase interferes with Trypanosoma cruzi infection and proliferation of the parasite.

Authors:  Salomé C Vilchez Larrea; Teemu Haikarainen; Mohit Narwal; Mariana Schlesinger; Harikanth Venkannagari; Mirtha M Flawiá; Silvia H Fernández Villamil; Lari Lehtiö
Journal:  PLoS One       Date:  2012-09-25       Impact factor: 3.240

10.  Structural basis and selectivity of tankyrase inhibition by a Wnt signaling inhibitor WIKI4.

Authors:  Teemu Haikarainen; Harikanth Venkannagari; Mohit Narwal; Ezeogo Obaji; Hao-Wei Lee; Yves Nkizinkiko; Lari Lehtiö
Journal:  PLoS One       Date:  2013-06-06       Impact factor: 3.240

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