Challenging the anticolorectal cancer capacity of quinoxaline-based scaffold via triazole ligation unveiled new efficient dual VEGFR-2/MAO-B inhibitors

Bioorganic Chemistry(2024)

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摘要
•Triazole-quinoxaline hybrids were crafted as dual VEGFR-2 /MAO-B inhibitors for halting CRC.•11 and 14 surpassed 5-FU against HCT-116cells regarding potency and selectivity.•14 recorded one-digit nanomolar IC50 concentration against VEGFR-2.•11 was superior to the reference MAOI methylene blue with MAO-B/A selectivity.•11 and 14 downregulated HIF-1α in HCT-116cells and inhibited their migration by ˃75 %.
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关键词
Colorectal cancer,Triazole,Quinoxaline,VEGFR-2,MAO-B/A selectivity
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