Taggi Andrew E, Stevenson Thomas M, Bereznak James F, Sharpe Paula L, Gutteridge Steven, Forman Robert, Bisaha John J, Cordova Daniel, Crompton Martina, Geist Lora, Kovacs Patrick, Marshall Eric, Sheth Ritesh, Stavis Courtney, Tseng Chi-Ping
DuPont Crop Protection, Discovery Chemistry, 1090 Elkton Road, Newark, DE 19714, USA.
DuPont Crop Protection, Discovery Chemistry, 1090 Elkton Road, Newark, DE 19714, USA.
Bioorg Med Chem. 2016 Feb 1;24(3):435-43. doi: 10.1016/j.bmc.2015.08.038. Epub 2015 Aug 28.
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.
已发现一类基于取代吡嗪 - 2 - 酮核心的新型合成微管蛋白聚合破坏剂。这些分子已被证明是强效的广谱杀菌剂,对农业上重要的子囊菌和担子菌病原体具有活性。还发现它们对人横纹肌肉瘤细胞特别有效。利用高效合成路线,对其农业和药用活性进行了探索。