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Discovery of novel sphingosine kinase-1 inhibitors. Part 2
Authors:Yibin Xiang  Bradford Hirth  John L Kane  Junkai Liao  Kevin D Noson  Christopher Yee  Gary Asmussen  Maria Fitzgerald  Christine Klaus  Michael Booker
Institution:1. Department of Medicinal Chemistry, Drug and Biomaterial R&D, Genzyme Corporation, 153 Second Avenue, Waltham, MA 02451, USA;2. Department of In Vitro Biology, Drug and Biomaterial R&D, Genzyme Corporation, 153 Second Avenue, Waltham, MA 02451, USA;3. Department of DMPK, Drug and Biomaterial R&D, Genzyme Corporation, 153 Second Avenue, Waltham, MA 02451, USA
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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