2. Academic Validation
  3. 5-Fluorocytosine derivatives as inhibitors of deoxycytidine kinase

5-Fluorocytosine derivatives as inhibitors of deoxycytidine kinase

  • Bioorg Med Chem Lett. 2009 Dec 1;19(23):6780-3. doi: 10.1016/j.bmcl.2009.09.082.
James E Tarver 1,  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
Affiliations

Affiliation

  • 1 Lexicon Pharmaceuticals, Princeton, NJ 08540, United States.
PMID: 19836229 DOI: 10.1016/j.bmcl.2009.09.082
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.

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