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

Zsolt Székelyhidi; János Pató; Frigyes Wáczek; Péter Bánhegyi; Bálint Hegymegi-Barakonyi; Dániel Erös; György Mészáros; Ferenc Hollósy; Doris Hafenbradl; Sabine Obert; Bert Klebl; György Kéri; László Orfi

doi:10.1016/j.bmcl.2005.04.064

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.

Authors

Zsolt Székelyhidi¹, János Pató, Frigyes Wáczek, Péter Bánhegyi, Bálint Hegymegi-Barakonyi, Dániel Erös, György Mészáros, Ferenc Hollósy, Doris Hafenbradl, Sabine Obert, Bert Klebl, György Kéri, László Orfi

Affiliation

¹ Peptide Biochemistry Res. Group of Hung. Acad. Sci. and Cooperative Research Centre, Semmelweis University, Rippl-Rónai u. 37., Budapest 1062, Hungary.

PMID: 15925511
DOI: 10.1016/j.bmcl.2005.04.064

Abstract

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

Substances

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