title: Synthesis of selective SRPK-1 inhibitors: novel tricyclic quinoxaline derivatives.
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.
authors.affiliation: Peptide Biochemistry Res. Group of Hung. Acad. Sci. and Cooperative Research Centre, Semmelweis University, Rippl-Rónai u. 37., Budapest 1062, Hungary.
authors.forename: Zsolt
authors.initials: Z
authors.lastname: Székelyhidi
authors.forename: János
authors.initials: J
authors.lastname: Pató
authors.forename: Frigyes
authors.initials: F
authors.lastname: Wáczek
authors.forename: Péter
authors.initials: P
authors.lastname: Bánhegyi
authors.forename: Bálint
authors.initials: B
authors.lastname: Hegymegi-Barakonyi
authors.forename: Dániel
authors.initials: D
authors.lastname: Erös
authors.forename: György
authors.initials: G
authors.lastname: Mészáros
authors.forename: Ferenc
authors.initials: F
authors.lastname: Hollósy
authors.forename: Doris
authors.initials: D
authors.lastname: Hafenbradl
authors.forename: Sabine
authors.initials: S
authors.lastname: Obert
authors.forename: Bert
authors.initials: B
authors.lastname: Klebl
authors.forename: György
authors.initials: G
authors.lastname: Kéri
authors.forename: László
authors.initials: L
authors.lastname: Orfi
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D006509:Hepatitis B / Q000188:drug therapy; D006515:Hepatitis B virus; D006801:Humans; D020128:Inhibitory Concentration 50; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000998:Antiviral Agents; D004791:Enzyme Inhibitors; D011810:Quinoxalines; C087728:SRPK1 protein, human; D017346:Protein Serine-Threonine Kinases