Abstract a series of benzodioxole compounds were synthesized and evaluated for their cytotoxic activity against cervical (Hela), colorectal (Caco-2), and liver (Hep3B) cancer cell lines. Compounds 5a, 5b, 6a, 6b, 7a and 7b showed very weak or negligible anticancer activity with IC50 3.94-9.12 mM. On the contrary, carboxamide containing compounds 2a and 2b showed anticancer activity. Both 2a and 2b reduced Hep3B secretions of α-fetoprotein (α-FP) to 1625.8 ng/ml and 2340 ng/ml, respectively, compared to 2519.17 ng/ml in untreated cells. The results also showed that compound 2a has potent anticancer activity against Hep3B cancer cell line. Furthermore, in cell cycle analysis, compound 2a induced arrest in the G2-M phase in value of 8.07% that was very close to the activity of doxorubicin (7.4%). These results indicate that compound 2a has a potent and promising antitumor activity. However, benzodiazepine derivatives (7a and 7b) showed moderate antioxidant activity with IC50 values of 39.85 and 79.95 μM, respectively compared with the potent antioxidant agent Trolox (IC50 = 7.72 μM).

中文翻译：

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苯并二氧杂环戊烯衍生物作为潜在抗癌和抗氧化剂的合成和生物学评价

摘要 合成了一系列苯并二氧杂环戊烯化合物，并评估了它们对宫颈癌 (Hela)、结肠直肠癌 (Caco-2) 和肝癌 (Hep3B) 癌细胞系的细胞毒活性。化合物 5a、5b、6a、6b、7a 和 7b 显示出非常弱或可忽略的抗癌活性，IC50 为 3.94-9.12 mM。相反，含有甲酰胺的化合物 2a 和 2b 显示出抗癌活性。与未处理细胞中的 2519.17 ng/ml 相比，2a 和 2b 将甲胎蛋白 (α-FP) 的 Hep3B 分泌分别降低至 1625.8 ng/ml 和 2340 ng/ml。结果还表明，化合物2a对Hep3B癌细胞系具有有效的抗癌活性。此外，在细胞周期分析中，化合物 2a 诱导的 G2-M 期阻滞值为 8.07%，非常接近阿霉素的活性 (7.4%)。这些结果表明化合物 2a 具有有效且有前景的抗肿瘤活性。然而，与强抗氧化剂 Trolox（IC50 = 7.72 μM）相比，苯二氮卓衍生物（7a 和 7b）显示出中等的抗氧化活性，IC50 值分别为 39.85 和 79.95 μM。