Design, synthesis, and biological evaluation of novel HDAC inhibitors with a 3-(benzazol-2-yl)quinoxaline framework
Bioorganic & Medicinal Chemistry Letters(2023)
摘要
•A series of novel histone deacetylase (HDAC) inhibitors based on 3-(benzazol-2-yl)quinoxaline derivatives were prepared.•10c displayed stronger anti-proliferative activity than SAHA against HCT-116 cells.•10c exhibited significant Topo I inhibition.•10c could induce apoptosis better than SAHA.•10c arrested the HCT-116 cells at G2/M phase.•10c induced activation of mitochondrial apoptosis signaling pathway related to the cancer cell inhibition.
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关键词
Epigenetics, Histone deacetylase, Topoisomerase I, Antitumor, Inhibitors
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