Discovery of novel sphingosine kinase-1 inhibitors. Part 2

  • Bioorg Med Chem Lett. 2010 Aug 1;20(15):4550-4. doi: 10.1016/j.bmcl.2010.06.019.
Yibin Xiang  1 ,  Bradford Hirth ,  John L Kane Jr ,  Junkai Liao ,  Kevin D Noson ,  Christopher Yee ,  Gary Asmussen ,  Maria Fitzgerald ,  Christine Klaus ,  Michael Booker
Affiliations
  • 1. Department of Medicinal Chemistry, Drug and Biomaterial R&D, Genzyme Corporation, Waltham, MA 02451, USA. [email protected]
PMID: 20598880 DOI: 10.1016/j.bmcl.2010.06.019
Abstract

Building on our initial work, we have identified additional novel inhibitors of sphingosine kinase-1 (SK1). These new analogs address the shortcomings found in our previously reported compounds. Inhibitors 51 and 54 demonstrated oral bioavailability in a rat PK study.

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