五味子呋喃糖苷 G 衍生物的设计、合成及其作为潜在抗癌剂的生物学评价

IF 1.5 4区化学 Q3 CHEMISTRY, ORGANIC Tetrahedron Letters Pub Date : 2024-08-06 DOI:10.1016/j.tetlet.2024.155244

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引用次数: 0

摘要

五味子呋喃素 G 是含有六氢噻吩分子的五味子呋喃素中最有效的一种，它对 A549 和 KB 细胞株具有很强的细胞毒性，IC50 值分别为 0.8 μM 和 0.6 μM。本文利用多组分反应从五味子呋喃糖 G 合成了一系列新的异戊烯基侧链修饰的五味子呋喃糖 G 衍生物。评估了所有合成化合物对四种人类癌细胞株（KB、Hep3B、A549、MCF7）和一种非癌细胞株（HEK293）的细胞毒性，从而对分子中仍未被充分探索的部分进行了深入的结构-活性关系研究。

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Design, synthesis of schweinfurthin G derivatives and their biological evaluation as potential anticancer agents

Schweinfurthin G, one of the most potent of the schweinfurthins containing a hexahydroxanthene moiety, was found to exhibit strong cytotoxicity against A549 and KB cell lines with the IC₅₀ values of 0.8 μM and 0.6 μM, respectively. In this paper, a new series of schweinfurthin G derivatives modified on the isoprenyl side-chain were synthesized from schweinfurthin G using multicomponent reactions. The cytotoxicity of all the synthetic compounds was evaluated against four human cancer cell lines (KB, Hep3B, A549, MCF7) and one non-cancerous cell line (HEK293), which enabled to perform in-depth structure–activity relationships on a still poorly explored part of the molecule.

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来源期刊

Tetrahedron Letters 化学-有机化学

CiteScore

3.50

自引率

5.60%

发文量

521

审稿时长

28 days

期刊介绍： Tetrahedron Letters provides maximum dissemination of outstanding developments in organic chemistry. The journal is published weekly and covers developments in techniques, structures, methods and conclusions in experimental and theoretical organic chemistry. Rapid publication of timely and significant research results enables researchers from all over the world to transmit quickly their new contributions to large, international audiences.