An ml210 derivative, its preparation method and application in preparing anti-tumor drugs

By introducing subcellular organelle targeting groups into ML210 derivatives, mitochondrial or lysosomal targeted GPX4 inhibitors were synthesized, solving the problem of poor water solubility of ML210, achieving efficient inhibition of tumor cells and optimizing drug distribution, and improving drug quality and safety.

CN122404246APending Publication Date: 2026-07-17DALIAN UNIV OF TECH
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Patent Information

Application Number
CN202610490710.X
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2026-04-14
Publication Date
2026-07-17

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Abstract

本发明公开了一种ML210衍生物及其制备方法和在制备抗肿瘤药物中的应用。该ML210衍生物对HT‑1080、MDA‑MB‑231和HeLa细胞均表现出一定的体外抗肿瘤活性。且相较于现有铁死亡诱导剂ML210，本发明的ML210衍生物在诱导肿瘤细胞铁死亡的同时，显著提高水溶性，有效改善了现有ML210成药性差等缺陷，具有良好的制备抗肿瘤药物的应用潜力。此外活性评价结果表明，线粒体靶向化合物与溶酶体靶向化合物的抑制效果总体相近，说明线粒体和溶酶体在铁死亡发生过程中均具有重要调控作用，二者在促进铁死亡方面未表现出明显差异。同时化合物能够在一定程度上较为特异性地诱导HT‑1080细胞发生铁死亡，本发明ML210衍生物具有较明确的作用机制，能够作为有潜力的抗肿瘤化合物用于抗肿瘤药物开发。
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