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Abstract <p>Erianin, despite its potent anticancer effects against various cancer cell lines, suffers from poor bioavailability due to limited solubility and rapid metabolism. To overcome these limitations, a series of novel erianin derivatives were designed, synthesized, and evaluated for their biological activities against HeLa, MDA-MB-231, and A498 cancer cell lines. Among these derivatives, compound <b>8j</b>, 4-[6,7-dimethoxy-3,4-dihydro­isoquinolin-2(1<i>H</i>)-yl]-<i>N</i>-(4-methoxybenzyl)-4-oxo-<i>N</i>-(3,4,5-trimethoxyphenyl)butanamide, demonstrated the highest selectivity and most potent activity against HeLa cells with an IC<sub>50</sub> value of 7.53±3.57 μM. Compound <b>8j</b> significantly inhibited the adhesion, proliferation, migration, and invasion of HeLa cells in a dose-dependent manner. Preliminary pharmacokinetic evaluations suggest favorable absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties consistent with drug-like behavior. Molecular docking studies further revealed that <b>8j</b> binds to the colchicine-binding site of tubulin, indicating its potential mechanism of action. These findings suggest that compound <b>8j</b> is a promising lead candidate for the development of novel anticancer agents targeting the colchicine-binding site on tubulin.</p>

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Design, Synthesis, and Antitumor Activity of Erianin Derivatives

  • 期刊论文

  • 发表日期：

    2025年4月1日

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  • Bailing Jiang,
  • Siqi Wang,
  • Caiju Wu,
  • Yifei Gu

摘要

Abstract

Erianin, despite its potent anticancer effects against various cancer cell lines, suffers from poor bioavailability due to limited solubility and rapid metabolism. To overcome these limitations, a series of novel erianin derivatives were designed, synthesized, and evaluated for their biological activities against HeLa, MDA-MB-231, and A498 cancer cell lines. Among these derivatives, compound 8j, 4-[6,7-dimethoxy-3,4-dihydro­isoquinolin-2(1H)-yl]-N-(4-methoxybenzyl)-4-oxo-N-(3,4,5-trimethoxyphenyl)butanamide, demonstrated the highest selectivity and most potent activity against HeLa cells with an IC50 value of 7.53±3.57 μM. Compound 8j significantly inhibited the adhesion, proliferation, migration, and invasion of HeLa cells in a dose-dependent manner. Preliminary pharmacokinetic evaluations suggest favorable absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties consistent with drug-like behavior. Molecular docking studies further revealed that 8j binds to the colchicine-binding site of tubulin, indicating its potential mechanism of action. These findings suggest that compound 8j is a promising lead candidate for the development of novel anticancer agents targeting the colchicine-binding site on tubulin.