title: Discovery of novel sphingosine kinase-1 inhibitors. Part 2.
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.
authors.affiliation: Department of Medicinal Chemistry, Drug and Biomaterial R&D, Genzyme Corporation, Waltham, MA 02451, USA. yibin.xiang@genzyme.com
authors.forename: Yibin
authors.initials: Y
authors.lastname: Xiang
authors.forename: Bradford
authors.initials: B
authors.lastname: Hirth
authors.forename: John L
authors.initials: JL
authors.lastname: Kane
authors.forename: Junkai
authors.initials: J
authors.lastname: Liao
authors.forename: Kevin D
authors.initials: KD
authors.lastname: Noson
authors.forename: Christopher
authors.initials: C
authors.lastname: Yee
authors.forename: Gary
authors.initials: G
authors.lastname: Asmussen
authors.forename: Maria
authors.initials: M
authors.lastname: Fitzgerald
authors.forename: Christine
authors.initials: C
authors.lastname: Klaus
authors.forename: Michael
authors.initials: M
authors.lastname: Booker
mesh_terms: D000818:Animals; D001547:Benzaldehydes / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D006801:Humans; D008094:Lithium / Q000737:chemistry*; D008862:Microsomes, Liver / Q000378:metabolism; D017853:Phosphotransferases (Alcohol Group Acceptor) / Q000037:antagonists & inhibitors* / Q000378:metabolism; D051381:Rats; D000099157:Sphingosine Kinase
chemical_list: D001547:Benzaldehydes; D004791:Enzyme Inhibitors; D008094:Lithium; D017853:Phosphotransferases (Alcohol Group Acceptor); D000099157:Sphingosine Kinase; C488327:4-cyanobenzaldehyde