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Bioorg Med Chem ; 24(3): 435-43, 2016 Feb 01.
Article in English | MEDLINE | ID: mdl-26386818

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.


Subject(s)
Antineoplastic Agents/pharmacology , Fungicides, Industrial/pharmacology , Pyrazines/pharmacology , Tubulin Modulators/chemistry , Tubulin Modulators/pharmacology , Tubulin/metabolism , Antineoplastic Agents/chemistry , Cell Line, Tumor , Cell Proliferation/drug effects , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Fungicides, Industrial/chemistry , Humans , Microbial Sensitivity Tests , Molecular Structure , Pyrazines/chemistry , Structure-Activity Relationship
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