Abstract

A series of lupeol derivatives 2, 2a-2f, 2a-2h, 3a-3e, and 4a-4b were designed, synthesised and evaluated for their α-glucosidase inhibitory and cytotoxic activities. Among synthetic derivatives, lupeol analogues 2b and 2e containing a benzylidene chain exhibited the best activity against α-glucosidase and superior to the positive agent with the IC₅₀ values of 29.4 ± 1.33 and 20.1 ± 0.91 μM, respectively. Lupeol analogues 2d and 3a showed weak cytotoxicity against K562 cell line with the IC₅₀ values of 76.6 ± 2.40 and 94.4 ± 1.51 μM, respectively.

中文翻译：

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新型羽扇豆醇衍生物的设计和合成及其α-葡萄糖苷酶抑制和细胞毒活性

摘要

一系列羽扇豆醇衍生物的2，图2A-2F，图2a-2H，3A-3E和4A-4B设计，合成并评价了它们的α葡萄糖苷酶抑制和细胞毒活性。在合成衍生物中，含有亚苄基链的羽扇豆醇类似物2b和2e对α-葡萄糖苷酶的活性最好，并且优于阳性试剂，IC ₅₀值分别为 29.4 ± 1.33 和 20.1 ± 0.91 μM。Lupeol 类似物2d和3a对 K562 细胞系显示出弱的细胞毒性，IC ₅₀ 值分别为 76.6 ± 2.40 和 94.4 ± 1.51 μM。