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Updated: May 22, 2026

A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English
Published on: April 3, 2026
The design, synthesis, and biological evaluation of PIM kinase inhibitors
Amy Lew Tsuhako1, David S Brown, Elena S Koltun
1Exelixis, Department of Drug Discovery, South San Francisco, CA 94080, USA. alew@exelixis.com
Abstract:
A series of substituted benzofuropyrimidinones with pan-PIM activities and excellent selectivity against a panel of diverse kinases is described. Initial exploration identified aryl benzofuropyrimidinones that were potent, but had cell permeability limitation. Using X-ray crystal structures of the bound PIM-1 complexes with 3, 5m, and 6d, we were able to guide the SAR and identify the alkyl benzofuropyrimidinone (6l) with good PIM potencies, permeability, and oral exposure.
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