| Literature DB >> 19836229 |
James E Tarver1, Theodore C Jessop, Marianne Carlsen, David J Augeri, Qinghong Fu, Jason P Healy, Alexander Heim-Riether, Amy Xu, Jerry A Taylor, Min Shen, Philip E Keyes, S David Kimball, Xuan-Chuan Yu, Maricar Miranda, Qingyun Liu, Jonathan C Swaffield, Amr Nouraldeen, Alan G E Wilson, Rick Finch, Kanchan Jhaver, Ann Marie Digeorge Foushee, Steve Anderson, Tamas Oravecz, Kenneth G Carson.
Abstract
A series of potent piperidine-linked cytosine derivatives were prepared as inhibitors of deoxycytidine kinase (dCK). Compound 9h was discovered to be a potent inhibitor of dCK and shows a good combination of cellular potency and pharmacokinetic parameters. Compound 9h blocks the incorporation of radiolabeled cytosine into mouse T-cells in vitro, as well as in vivo in mice following a T-cell challenge.Entities:
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Year: 2009 PMID： 19836229 DOI： 10.1016/j.bmcl.2009.09.082
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823