Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1374912 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
A series of deoxycytidine kinase inhibitors was simultaneously optimized for potency and PK properties. A co-crystal structure then allowed merging this series with a high throughput screening hit to afford a highly potent, selective and orally bioavailable inhibitor, compound 10. This compound showed dose dependent inhibition of deoxycytidine kinase in vivo.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Theodore C. Jessop, James E. Tarver, Marianne Carlsen, Amy Xu, Jason P. Healy, Alexander Heim-Riether, Qinghong Fu, Jerry A. Taylor, David J. Augeri, Min Shen, Terry R. Stouch, Ronald V. Swanson, Leslie W. Tari, Michael Hunter, Isaac Hoffman,