Synthesis of selective SRPK-1 inhibitors: novel tricyclic quinoxaline derivatives

Bioorg Med Chem Lett. 2005 Jul 1;15(13):3241-6. doi: 10.1016/j.bmcl.2005.04.064.


SR protein-specific kinase-1 (SRPK-1) has been identified as a validated target for hepatitis B virus (HBV). A series of novel tricyclic quinoxaline derivatives was designed and synthesised as potential kinase inhibitory antiviral agents and was found to be active and selective for SRPK-1 kinase. Most of these novel compounds have drug-like properties according to experimentally determined LogP and LogS values.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / pharmacology
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / pharmacology
  • Hepatitis B / drug therapy
  • Hepatitis B virus
  • Humans
  • Inhibitory Concentration 50
  • Protein Serine-Threonine Kinases / antagonists & inhibitors*
  • Quinoxalines / chemical synthesis*
  • Quinoxalines / pharmacology
  • Structure-Activity Relationship


  • Antiviral Agents
  • Enzyme Inhibitors
  • Quinoxalines
  • SRPK1 protein, human
  • Protein Serine-Threonine Kinases