Discovery research efforts at Corteva Agriscience inspired by literature reports on protein kinase inhibitors in combination with scaffold hopping exercises led to the identification of novel pyrimidinyl-based kinase herbicides bearing acylsulfonamides, carboxylates and amide sidechains that exhibited pre-emergent and post-emergent herbicidal activity. A systematic SAR was developed and a correlation of kinase inhibition and herbicidal activity was demonstrated. The most promising herbicides in this series of compounds exhibited highly promiscuous kinase inhibitory activity which included strong inhibitory activity towards Aurora A, FGFR1, and JAK. Accordingly, research focus was placed in understanding their mode of action and sustainability profile.

Discovery of pyrimidinyl-based kinase herbicides

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ACS Fall 2022

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