Abstract

Osthol [7-methoxy-8-(3-methylbut-2-en-1-yl)chromen-2-one] isolated from Prangos pabularia was used as a starting material for the synthesis of its various derivatives via modifications of the lactone ring. The resulting compounds were fully characterized by spectral techniques and evaluated for their anticancer activity against Hep-G2 (human hepatoma), HeLa (cervical carcinoma), U-87 (brain cancer) and MCF-7 (breast cancer) cell lines using MTT assay. All synthesized derivatives exhibited higher activity than that of osthol. Among this series, 4-bromophenyl, 3-hydroxyphenyl, and p-tolyl derivatives showed excellent cytotoxic activity against U-87 and MCF-7 cancer cell lines with IC₅₀ values of 6–7.3 µM.

中文翻译：

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雌二醇新三唑衍生物的合成、表征和细胞毒性评价

摘要

从Prangos pabularia中分离出的 Osthol [7-methoxy-8-(3-methylbut-2-en-1-yl) chromen -2-one]用作起始材料，通过内酯环的修饰合成其各种衍生物. 所得化合物通过光谱技术进行了全面表征，并使用 MTT 测定评估了它们对 Hep-G2（人肝癌）、HeLa（宫颈癌）、U-87（脑癌）和 MCF-7（乳腺癌）细胞系的抗癌活性. 所有合成的衍生物都表现出比蛇床素更高的活性。在该系列中，4-溴苯基、3-羟基苯基和对甲苯基衍生物对 U-87 和 MCF-7 癌细胞系显示出优异的细胞毒活性，IC ₅₀值为 6–7.3 µM。