Synthesis of selective SRPK-1 inhibitors: novel tricyclic quinoxaline derivatives.
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.
Székelyhidi
Zsolt
Z
Peptide Biochemistry Res. Group of Hung. Acad. Sci. and Cooperative Research Centre, Semmelweis University, Rippl-Rónai u. 37., Budapest 1062, Hungary.
Pató
János
J
Wáczek
Frigyes
F
Bánhegyi
Péter
P
Hegymegi-Barakonyi
Bálint
B
Erös
Dániel
D
Mészáros
György
G
Hollósy
Ferenc
F
Hafenbradl
Doris
D
Obert
Sabine
S
Klebl
Bert
B
Kéri
György
G
Orfi
László
L
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
D000998:Antiviral Agents; D004791:Enzyme Inhibitors; D011810:Quinoxalines; C087728:SRPK1 protein, human; D017346:Protein Serine-Threonine Kinases