Department of Chemistry, Faculty of Science, King Saud University, P. O. Box 2455, Riyadh 11451, Saudi Arabia.
Int J Mol Sci. 2013 Mar 12;14(3):5712-22. doi: 10.3390/ijms14035712.
Thioenethiophene derivatives represent an important class of compounds with diverse biological activities. We describe here the synthesis of a new series of thieno[2,3-b]thiophene containing bis-heterocyclic compounds 3-7. All the compounds were evaluated for their in vitro antioxidant potential, α-glucosidase and β-glucuronidase inhibiton and anticancer activity against PC-3 cell lines. Compounds 2b (IC50 = 1.3 ± 0.2 μM), 5a (IC50 = 2.3 ± 0.4 μM) and 5b (IC50 = 8.7 ± 0.1 μM) showed a potent inhibition of β-glucuronidase enzyme, more active than the standard d-saccharic acid 1,4-lactone (IC50 = 45.8 ± 2.5 μM). Compounds 5a (IC50 = 22.0 ± 0.3 μM) and 5b (IC50 = 58.4 ± 1.2 μM) were also found to be potent α-glucosidase inhibitors as compared to standard drug (acarbose, IC50 = 841 ± 1.7 μM).
噻吩并[2,3-b]噻吩衍生物是一类具有多种生物活性的重要化合物。我们在这里描述了一系列新的含双杂环化合物 3-7 的噻吩并[2,3-b]噻吩的合成。所有化合物均进行了体外抗氧化活性、α-葡萄糖苷酶和β-葡萄糖醛酸酶抑制活性以及对 PC-3 细胞系的抗癌活性评价。化合物 2b（IC50 = 1.3 ± 0.2 μM）、5a（IC50 = 2.3 ± 0.4 μM）和 5b（IC50 = 8.7 ± 0.1 μM）对β-葡萄糖醛酸酶表现出很强的抑制作用，比标准的 d-酒石酸 1,4-内酯（IC50 = 45.8 ± 2.5 μM）更有效。与标准药物（阿卡波糖，IC50 = 841 ± 1.7 μM）相比，化合物 5a（IC50 = 22.0 ± 0.3 μM）和 5b（IC50 = 58.4 ± 1.2 μM）也被发现是有效的α-葡萄糖苷酶抑制剂。
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