sphingosine-kinase has been researched along with pyrrolidine* in 2 studies
2 other study(ies) available for sphingosine-kinase and pyrrolidine
| Article | Year |
|---|---|
Evaluation of pyrrolidine-based analog of jaspine B as potential SphK1 inhibitors against rheumatoid arthritis.
Rheumatoid arthritis (RA) is a chronic autoimmune disease characterized by synovitise, and its pathogenesis is complicated. Sphingosine-1-phosphate (S1P) is a lipid produced by sphingosine kinase 1 and 2 (SphK1/2), which participate in some of most-spread skeletal diseases such as rheumatoid arthritis or osteoarthritis. To explore the anti-inflammatory activity of 2-epi-jaspine B analogs as SphKs inhibitors, we used LPS-induced rheumatoid arthritis fibroblast-like synovial cells (HFLS-RA) as the research object to evaluate the anti-inflammatory activity of 16 2-epi-jaspine B analogs and the newly synthesized salt CHJ01. We found that 2-epi-jaspine B analog CHJ01 in hydrochloride salt form has excellent SphK1 inhibitory effect and better anti-RA effect. CHJ01 showed an anti-inflammatory effect similar to that of MTX in vitro, its IC Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Arthritis, Rheumatoid; Dose-Response Relationship, Drug; Enzyme Inhibitors; Freund's Adjuvant; Molecular Structure; Phosphotransferases (Alcohol Group Acceptor); Pyrrolidines; Rats; Sphingosine; Structure-Activity Relationship | 2021 |
Discovery of a Potent and Selective Sphingosine Kinase 1 Inhibitor through the Molecular Combination of Chemotype-Distinct Screening Hits.
Topics: Amination; Benzimidazoles; Drug Discovery; Humans; Models, Molecular; Phosphotransferases (Alcohol Group Acceptor); Protein Kinase Inhibitors; Pyrrolidines | 2017 |