2. Academic Validation
  3. Tubulin modulating antifungal and antiproliferative pyrazinone derivatives

Tubulin modulating antifungal and antiproliferative pyrazinone derivatives

  • Bioorg Med Chem. 2016 Feb 1;24(3):435-43. doi: 10.1016/j.bmc.2015.08.038.
Andrew E Taggi 1,  Thomas M Stevenson 2,  James F Bereznak 2,  Paula L Sharpe 2,  Steven Gutteridge 3,  Robert Forman 4,  John J Bisaha 2,  Daniel Cordova 3,  Martina Crompton 4,  Lora Geist 2,  Patrick Kovacs 2,  Eric Marshall 2,  Ritesh Sheth 2,  Courtney Stavis 2,  Chi-Ping Tseng 2
Affiliations

Affiliations

  • 1 DuPont Crop Protection, Discovery Chemistry, 1090 Elkton Road, Newark, DE 19714, USA. Electronic address: andrew.e.taggi@dupont.com.
  • 2 DuPont Crop Protection, Discovery Chemistry, 1090 Elkton Road, Newark, DE 19714, USA.
  • 3 DuPont Crop Protection, Chemical Genomics, 1090 Elkton Road, Newark, DE 19714, USA.
  • 4 DuPont Crop Protection, Discovery Biology, 1090 Elkton Road, Newark, DE 19714, USA.
PMID: 26386818 DOI: 10.1016/j.bmc.2015.08.038
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.

Keywords

Agriculture; Cell line; Fungicide; Pathogen; Synthesis; Tubulin.

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