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蒂亚迪亚佐尔,塞莱纳迪亚佐尔和三醇结合的 antraquinones 作为G-quadruplex 向的抗癌化合物

Daria V Andreeva¹, Tatiana S Vedekhina², Alexander S Gostev³

¹Gause Institute of New Antibiotics, 11 B. Pirogovskaya Street, Moscow, 119021, Russia.

European journal of medicinal chemistry

|February 22, 2024

概括

这项研究合成了用于癌症治疗的新型G-quadruplex (G4) 配体. 提亚二和二衍生物有效地抑制了瘤细胞的增殖和稳定了G4结构,显示出作为抗癌剂的前景.

科学领域:

药用化学医学化学
在瘤学瘤学.
分子生物学分子生物学

背景情况:

作为潜在的抗癌疗法,G-四重复 (G4) 配体正在被研究.
开发具有提高疗效和特异性的新型G4配体对于癌症治疗至关重要.

研究的目的:

为了合成新型的合醇的氨衍生物作为G4配体.
评估它们与G4形成的寡核酸结合的亲和力,细胞积累和抗瘤功效.
调查这些新型G4连接体的结构-活性关系.

主要方法:

用不同的侧链合成与醇结合的氨酸.
使用G4形成的寡核酸 (端粒和c-MYC) 进行G4联体结合试验.
细胞增殖试验 (例如,K562白血病细胞).
西部涂抹以评估c-MYC瘤基因表达.
细胞周期分析和细胞亡测定.

主要成果:

基于蒂亚迪亚和塞莱纳迪亚的配体显示出显著抑制瘤细胞增殖.
这些配体有效地稳定了端粒和c-MYC G4 结构.
乙二醇衍生物11a在体外对c-MYC G4具有很高的亲和力,并且在细胞中减少了c-MYC瘤基因表达.
素11a诱导剂量和时间依赖的细胞周期停止和细胞亡,抑制K562细胞生长.

结论:

在G4配体中,密切相关的异环结构可以显著影响它们的生物特性.
蒂亚迪亚佐尔和塞莱纳迪亚佐尔化的人类素是开发针对G4结构的新型抗癌疗法的有希望的支架.
炭二醇衍生物11a通过向c-MYC G4.4显示出作为有效抗K562白血病剂的潜力.

关键词:

人类氨酸 (Anthraquinone) 是一种它具有抗癌活性.亚醇是一种醇.在G-quadruplex中使用.异循环是指异循环的.细胞内积累的细胞内积累.核酸是核酸中的一种.c-MYCC 这是一个很好的例子.

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