Literature DB >> 26386818

Tubulin modulating antifungal and antiproliferative pyrazinone derivatives.

Andrew E Taggi1, Thomas M Stevenson2, James F Bereznak2, Paula L Sharpe2, Steven Gutteridge3, Robert Forman4, John J Bisaha2, Daniel Cordova3, Martina Crompton4, Lora Geist2, Patrick Kovacs2, Eric Marshall2, Ritesh Sheth2, Courtney Stavis2, Chi-Ping Tseng2.   

Abstract

A novel class of synthetic tubulin polymerization disruptors, based on a substituted pyrazin-2-one core, has been discovered. These molecules have proven to be potent broad spectrum fungicides, with activity on agriculturally important ascomycete and basidiomycete pathogens. They have also been found to be particularly potent against human rhabdomyosarcoma cells. Using an efficient synthetic route, the agricultural and medicinal activity was explored.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Agriculture; Cell line; Fungicide; Pathogen; Synthesis; Tubulin

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Year:  2015        PMID: 26386818     DOI: 10.1016/j.bmc.2015.08.038

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  2 in total

Review 1.  Non-Naturally Occurring Small Molecule Microtubule-Stabilizing Agents: A Potential Tactic for CNS-Directed Therapies.

Authors:  Carlo Ballatore; Kurt R Brunden; John Q Trojanowski; Virginia M-Y Lee; Amos B Smith
Journal:  ACS Chem Neurosci       Date:  2016-11-29       Impact factor: 4.418

2.  Nucleophilic and electrophilic cyclization of N-alkyne-substituted pyrrole derivatives: Synthesis of pyrrolopyrazinone, pyrrolotriazinone, and pyrrolooxazinone moieties.

Authors:  Işıl Yenice; Sinan Basceken; Metin Balci
Journal:  Beilstein J Org Chem       Date:  2017-05-04       Impact factor: 2.883

  2 in total

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