Liang Jia-Hua, Cho Shu-Tse, Shih Tzenge-Lien, Chen Jih-Jung
Institute of Traditional Medicine, National Yang Ming Chiao Tung University Taipei 112304 Taiwan
Department of Chemistry, Tamkang University 251301 Tamsui Dist. New Taipei City Taiwan
RSC Adv. 2024 Sep 9;14(39):28659-28668. doi: 10.1039/d4ra04453c. eCollection 2024 Sep 4.
Twenty-six quinoxalin derivatives were synthesized to assess their biological activities against human non-small-cell lung cancer cells (A549 cells). Compound 4b (IC = 11.98 ± 2.59 μM) and compound 4m (IC = 9.32 ± 1.56 μM) possess anticancer activity comparable to 5-fluorouracil (clinical anticancer drug) (IC = 4.89 ± 0.20 μM). Western blot tests further confirmed that compound 4m effectively induced apoptosis of A549 cells through mitochondrial- and caspase-3-dependent pathways. The introduction of bromo groups instead of nitro groups into the quinoxaline skeleton has been shown to provide better inhibition against lung cancer cells in this article. This modification in the molecular structure could enhance the biological activity and effectiveness of quinoxaline derivatives in the design and synthesis of anticancer drugs, making bromo-substituted quinoxalines a promising avenue for further research and development in anticancer therapeutics.
合成了26种喹喔啉衍生物，以评估它们对人非小细胞肺癌细胞（A549细胞）的生物活性。化合物4b（IC = 11.98±2.59μM）和化合物4m（IC = 9.32±1.56μM）具有与5-氟尿嘧啶（临床抗癌药物）相当的抗癌活性（IC = 4.89±0.20μM）。蛋白质印迹试验进一步证实，化合物4m通过线粒体和半胱天冬酶-3依赖性途径有效诱导A549细胞凋亡。本文表明，在喹喔啉骨架中引入溴基团而非硝基可对肺癌细胞提供更好的抑制作用。这种分子结构的修饰可以增强喹喔啉衍生物在抗癌药物设计和合成中的生物活性和有效性，使溴代喹喔啉成为抗癌治疗进一步研发的有前景途径。
