| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374068 | Bioorganic & Medicinal Chemistry Letters | 2012 | 7 Pages |
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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Related Topics
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Chemistry
Organic Chemistry
Authors
Amy Lew Tsuhako, David S. Brown, Elena S. Koltun, Naing Aay, Arlyn Arcalas, Vicky Chan, Hongwang Du, Stefan Engst, Maurizio Franzini, Adam Galan, Ping Huang, Stuart Johnston, Brian Kane, Moon H. Kim, A. Douglas Laird, Rui Lin, Lillian Mock, Iris Ngan,