Among the family of nitrogen-containing heterocycles, quinoxalinone (or quinoxalin-2-one)
core, characterized by pyrazin-2(1H)-one fused to benzene ring at two adjacent carbon atoms, has been
frequently found in a variety of pharmacologically active compounds with biological or pharmaceutical
applications. It was gratifying that a larger part of these bioactive quinoxalinone-based derivatives
has entered various clinical trials, which in turn hastens the synthetic versatility and also initiates various
derivatization of quinoxalinone scaffold. In this review, we highlighted the newly emerged quinoxalinone-
based derivatives or analogues, with the emphasis of their biological applications and
structure-activity analysis covering literatures in recent years.
Keywords: Binding mode, biological activities, derivates, quinoxaline, quinoxalinone skeleton, SAR analysis.
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