Tubulin modulating antifungal and antiproliferative pyrazinone derivatives

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• 作者：Andrew E. Taggi^a ; ^{andrew.e.taggi@dupont.com" class="auth_mail" title="E-mail the corresponding author} ; Thomas M. Stevenson^a ; James F. Bereznak^a ; Paula L. Sharpe^a ; Steven Gutteridge^b ; Robert Forman^c ; John J. Bisaha^a ; Daniel Cordova^b ; Martina Crompton^c ; Lora Geist^a ; Patrick Kovacs^a ; Eric Marshall^a ; Ritesh Sheth^a ; Courtney Stavis^a ; Chi-Ping Tseng^a
• 关键词：Fungicide ; Tubulin ; Pathogen ; Synthesis ; Cell line ; Agriculture
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2016
• 出版时间：1 February 2016
• 年：2016
• 卷：24
• 期：3
• 页码：435-443
• 全文大小：1047 K

文摘

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.