1. Discovery of novel sphingosine kinase-1 inhibitors. Part 2.
- Author
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Xiang Y, Hirth B, Kane JL Jr, Liao J, Noson KD, Yee C, Asmussen G, Fitzgerald M, Klaus C, and Booker M
- Subjects
- Animals, Benzaldehydes chemical synthesis, Benzaldehydes pharmacokinetics, Drug Evaluation, Preclinical, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors pharmacokinetics, Humans, Microsomes, Liver metabolism, Phosphotransferases (Alcohol Group Acceptor) metabolism, Rats, Benzaldehydes chemistry, Enzyme Inhibitors chemistry, Lithium chemistry, Phosphotransferases (Alcohol Group Acceptor) antagonists & inhibitors
- 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., (Published by Elsevier Ltd.)
- Published
- 2010
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