Abstract

Series of novel N-benzyl derivatives of 6-aminoflavone (9a–n) were synthesized and evaluated for anticancer and topoisomerase II enzyme inhibition activity. All the synthesized compounds were screened for in vitro anticancer activity against human breast cancer cell line (MCF-7) and human lung cancer cell line (A-549). Among the synthesized compounds, 9f and 9g were found to be the most potent anticancer agents against human breast cancer cell line (MCF-7) with IC₅₀ values of 9.35 µM and 9.58 µM, respectively. Compounds 9b, 9c and 9n exhibited promising anticancer activity against human lung cancer cell line (A-549) with 43.71%, 46.48% and 44.26% inhibition at the highest concentration of 10 µM, respectively. Compounds 9c, 9f and 9g have ability to inhibit the topoisomerase II enzyme. Compound 9f showed most potent topoisomerase II enzyme inhibition activity with IC₅₀ value of 12.11 µM. Further, these compounds have a high potential to be developed as a promising topoisomerase II inhibitors.

中文翻译：

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通过还原胺化作用对 6-氨基黄酮进行 N-苄基化，并通过拓扑异构酶 II 抑制有效获得一些新型抗癌药物

摘要

合成了 6-氨基黄酮 ( 9a – n ) 的一系列新型N-苄基衍生物，并评估了其抗癌和拓扑异构酶 II 酶抑制活性。筛选所有合成的化合物对人乳腺癌细胞系 (MCF-7) 和人肺癌细胞系 (A-549) 的体外抗癌活性。在合成的化合物中，发现9f和9g是最有效的抗人乳腺癌细胞系 (MCF-7) 的抗癌剂，其 IC ₅₀值分别为 9.35 µM 和 9.58 µM。化合物9b、9c和9n对人肺癌细胞系 (A-549) 表现出有希望的抗癌活性，在 10 µM 的最高浓度下分别具有 43.71%、46.48% 和 44.26% 的抑制作用。化合物9c、9f和9g具有抑制拓扑异构酶II酶的能力。化合物9f显示出最有效的拓扑异构酶 II 酶抑制活性，IC ₅₀值为 12.11 µM。此外，这些化合物具有被开发为有前景的拓扑异构酶 II 抑制剂的巨大潜力。