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设计,合成和抗瘤活动含有氨酸组合的氨酸衍生物含氨酸组合

Wenting Zhang^1,2, Jian Sun¹, Peng Zhang²

¹Xuzhou Institute of Agricultural Sciences in Jiangsu Xuhuai District, Xuzhou 221131, China.

Molecules (Basel, Switzerland)

|January 11, 2024

概括

研究人员合成了新的氨酸衍生物,其中化合物3e通过诱导亡,通过诱导亡,对人类肝癌细胞 (HepG-2) 产生强烈的抑制作用,其性能优于西斯.

科学领域:

药用化学医学化学
有机合成有机合成
癌症研究癌症研究

背景情况:

奎尔是一种天然的黄类化合物,具有显著的生物和药理性质.
修改奎尔丁的3-OH位置可以导致具有增强治疗潜力的新衍生物.
开发新的抗癌药物对于治疗肝癌至关重要.

研究的目的:

为了合成新型氨酸衍生物,其中包含氨酸部分.
为了评估这些衍生物的体外抗癌活性对人类肝癌 (HepG-2) 细胞.
为了研究最强大的衍生品的作用机制.

主要方法:

鲁丁被用作瑞衍生物合成的起始材料.
化学修饰涉及甲基保护,威廉森乙化和替代反应.
合成化合物的表征使用1H NMR,13C NMR,IR和HRMS进行.
在体外细胞毒性使用IC50测定对HepG-2细胞进行了评估.
诱导亡被研究为一种作用机制.

主要成果:

成功合成和鉴定了15种含有诺林部分的瑞新型衍生物.
化合物3e对HepG-2细胞具有显著的抑制活性,IC50为6.722μmol·L-1.1.
与DDP (cisplatin) 相比,3e化合物表现出更高的疗效 (IC50 = 26.981 μmol·L-1).
机制研究表明,3e化合物会在HepG-2细胞中诱导细胞亡.

结论:

合成了新的氨酸-氨酸混合物,提供了一种新型的潜在抗癌剂.
化合物3e对人类肝癌具有有前途的抗癌活性,需要进一步研究.
诱导亡是化合物3e发挥细胞毒性作用的关键机制.

关键词:

它具有抗瘤活性.文素 (Quercetin) 是一种文素.昆氨酸 (quinoline) 是一种氨酸.综合合成是一种合成.

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