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Merck

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

Bioorganic & medicinal chemistry letters (2005-06-01)
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
RÉSUMÉ

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.

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