Abstract

Two new (−)-epigallocatechin-3-gallate-4β-triazolopodophyllotoxin conjugates (7 and 8) were synthesized and evaluated for biological activity. Compound 8 showed highly potent anticancer activity against A-549 cell line with IC₅₀ of 2.16 ± 1.02 μM, which displayed the highest selectivity index value (SI = 14.5) in A-549 cells. Molecular docking indicated that compound 8 could bind with the active site of Top-II. Therefore, compound 8 might be a promising candidate for further development.

中文翻译：

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(-)-epigallocatechin-3-gallate-4β-triazolopodophyllotoxin 偶联物的合成、抗肿瘤活性和分子对接

摘要

合成了两种新的 (-)-epigallocatechin-3-gallate-4β-triazolopodophyllotoxin 缀合物（7和8）并评估了其生物活性。化合物8对 A-549 细胞系显示出高效的抗癌活性，IC ₅₀为 2.16 ± 1.02 μM，在 A-549 细胞中显示出最高的选择性指数值 (SI = 14.5)。分子对接表明化合物8可以与Top-II的活性位点结合。因此，化合物8可能是进一步开发的有希望的候选者。