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作为抗瘤剂的 Cordycepin 衍生物的设计,合成和评估

Linlin Cui¹, Zheng Xu¹, Yu Zhu¹

¹College of Pharmacy, Harbin University of Commerce, Harbin, People's Republic of China.

Chemistry & biodiversity

|October 4, 2025

概括

合成和测试了具有尿素组的新型cordycepin衍生物的抗瘤特性. 化合物4l显示出显著的肝癌细胞抑制,诱导细胞亡和细胞循环停止,显示出治疗潜力.

科学领域:

药用化学医学化学
药理学药理学是指药理学的学科.
癌症生物学癌症生物学

背景情况:

科尔迪塞是一种具有已知的抗瘤活性的天然产品.
开发更强大的天然产品衍生品对于癌症治疗至关重要.
尿素功能化提供了一种提高药物疗效的策略.

研究的目的:

设计和合成包含尿素组的新型cordycepin衍生物.
评估这些衍生品的体外抗瘤疗效.
为了研究有前途的化合物的作用机制.

主要方法:

合成康迪塞-尿素衍生物.
使用IR,NMR,HPLC和HRMS进行结构性表征.
在体外细胞毒性测定 (MTT) 对癌细胞系 (MCF-7,HepG-2,SGC-7901,HK-2).
亡测定,细胞循环分析和西部抹杀.
分子对接模拟. 分子对接模拟.

主要成果:

几种新型cordycepin衍生物成功合成和表征.
化合物4l显示出对HepG-2肝癌细胞的显著抑制作用 (IC50 = 14.86 ± 2.37 μM),超过了cordycepin.
化合物4l诱导了亡,在G0/G1阶段停止了细胞循环,并激活了线粒体通路.
分子对接为化合物4l的结合相互作用提供了洞察力.

结论:

化合物4l是一种新型cordycepin衍生物,对肝癌细胞表现出强大的抗瘤活性.
该机制涉及通过线粒体通路诱导亡和细胞循环停止.
化合物4l是进一步开发肝癌治疗的有希望的候选物.

关键词:

这是一种抗瘤药物.灭症 (apoptosis) 是一种死亡的过程.科尔迪塞宾的衍生品.结构上的修改.尿素 urea 的使用方法

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