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A high-throughput screening (HTS) campaign identified a class of heteroaryl piperazines with excellent baseline affinity and selectivity for phosphoinositide 3-kinase δ (PI3Kδ) over closely related isoforms. Rapid evaluation and optimization of structure-activity relationships (SAR) for this class, leveraging the modular nature of this scaffold, facilitated development of this hit class into a series of potent and selective inhibitors of PI3Kδ. This effort culminated in the identification of 29, which displayed excellent potency in enzyme and cell-based assays, as well as favorable pharmacokinetic and off-target profiles. Copyright © 2019 Elsevier Ltd. All rights reserved.


Hua Zhou, Meredeth A McGowan, Kathryn Lipford, Matthew Christopher, Xavier Fradera, David Witter, Charles A Lesburg, Chaomin Li, Joey L Methot, John Lampe, Abdelghani Achab, Lynsey Shaffer, Peter Goldenblatt, Sanjiv Shah, Alan Bass, Gottfried Schroeder, Dapeng Chen, Haoyu Zeng, Martin A Augustin, Jason D Katz. Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors. Bioorganic & medicinal chemistry letters. 2020 Jan 01;30(1):126715

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PMID: 31757666

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