A novel series of dihydropyrano[3,2-c]quinoline derivatives 6a–q were synthesized and evaluated for their in vitro α-glucosidase inhibitory activities. All newly synthesized compounds displayed potent α-glucosidase inhibitory activity in the range of 10.3 ± 0.3 µM–172.5 ± 0.8 µM against the yeast α-glucosidase enzyme when compared to the standard drug acarbose (IC₅₀ = 750.0 ± 1.5 µM). Among these compounds, compounds 6e and 6d displayed the most potent α-glucosidase inhibitory activity (IC₅₀ = 10.3 ± 0.3 and 15.7 ± 0.5 µM, respectively). The kinetic analysis of the most potent compounds 6e and 6d revealed that compound 6e inhibited α-glucosidase in an uncompetitive manner (K_i = 11 µM) while compound 6d was a non-competitive inhibitor (K_i = 28 µM) of the enzyme. Then, the cytotoxicity of the most potent compounds (i.e., compounds 6a, 6d, 6e, 6 g, 6j, and 6l) were evaluated for toxicity using the breast cancer cell lines MDA-MB231, MCF-7, and T-47D by using a MTT assay, and no toxicity was observed.

合成了一系列新颖的二氢吡喃并[3,2-c]喹啉衍生物6a-q，并对其体外α-葡萄糖苷酶的抑制活性进行了评估。与标准药物阿卡波糖（IC ₅₀  = 750.0±1.5 µM）相比，所有新合成的化合物均对酵母α-葡萄糖苷酶表现出有效的α-葡萄糖苷酶抑制活性，范围为10.3±0.3 µM–172.5±0.8 µM 。在这些化合物中，化合物6e和6d表现出最强的α-葡萄糖苷酶抑制活性（IC _50分别 为10.3±0.3和15.7±0.5 µM）。对最有效的化合物6e和6d进行的动力学分析表明，该化合物6e以非竞争性方式抑制α-葡萄糖苷酶（K _i  = 11 µM），而化合物6d是 该酶的非竞争性抑制剂（K _i = 28 µM）。然后，使用MDA-MB231，MCF-7和T-47D乳腺癌细胞系评估最有效的化合物（即化合物6a，6d，6e，6 g，6j和6l）的细胞毒性，通过使用MTT测定法，未观察到毒性。