| Literature DB >> 19836232 |
Theodore C Jessop1, 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, Philip E Keyes, Xuan-Chuan Yu, Maricar Miranda, Qingyun Liu, Jonathan C Swaffield, S David Kimball, Amr Nouraldeen, Alan G E Wilson, Ann Marie Digeorge Foushee, Kanchan Jhaver, Rick Finch, Steve Anderson, Tamas Oravecz, Kenneth G Carson.
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.Mesh：
Substances：
Year: 2009 PMID： 19836232 DOI： 10.1016/j.bmcl.2009.09.081
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823