三种含有pyrimidylanthrahydrazone配体的 (II) 复合物:合成,晶体结构,DNA结合,抗癌活性和结构-活性关系
Jia-Yu Xu1, Xue-Bin Bi1, Sha-Sha Luo1
1Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education of China), Guangxi Key Laboratory of Chemistry and Molecular Engineering of Medicinal Resources, University Engineering Research Center for Chemistry of Characteristic Medicinal Resources (Guangxi), School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin 541004, China.
Journal of inorganic biochemistry
|December 3, 2025
概括
合成了三种新的 (II) 复合物,并对抗癌性质进行了评估. 9-PMAH-Co复合物显示出显著的DNA相互作用,拓酶I抑制,以及对癌细胞的强有力的细胞毒性,对正常细胞的毒性降低.
科学领域:
- 无机化学 无机化学
- 药用化学 医学化学
- 分子生物学分子生物学
背景情况:
- 开发新的基于金属的抗癌剂对于克服药物耐药性至关重要.
- 复合物已经显示出作为治疗剂的前景.
- 胺基甲氨配体提供了多样化的协调可能性.
研究的目的:
- 为了设计,合成和表征新的pyrimidylanthrahydrazone (II) 复合物.
- 为了评估它们的DNA相互作用,拓酶I抑制,以及体外抗癌活动.
- 研究它们的作用机制,包括细胞循环停止.
主要方法:
- 单晶X射线衍射用于结构确定.
- 用于DNA相互作用研究的光谱方法.
- 拓糖酶I抑制试验.
- 针对癌症和正常细胞系的体外抗增殖试验.
- 细胞周期分析.
主要成果:
- 三种六坐标单核 (((II) 复合物 (9-MPMAH-Co,9-FPMAH-Co,9-PMAH-Co) 被合成并进行了表征.
- 所有复合物都表现出DNA间隔,其中9-PMAH-Co在1μM时显示出显著的拓酶I抑制.
- 9-PMAH-Co对SK-OV-3和HeLa-229细胞表现出强烈的细胞毒性 (IC50值分别为4.99微米和8.09微米),并在SK-OV-3细胞中诱导了G2/M相停止.
- 在正常的肝细胞 (HL-7702) 中,与西斯相比,观察到毒性降低.
结论:
- 合成的复合体显示出有前途的抗癌活性.
- 9-PMAH-Co因其强大的细胞毒性作用和有利的毒性概况而被确定为一种化合物.
- 连接物替代物的结构性修改显著影响了复合物的生物活性.
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