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设计,合成和计算验证新型西醇衍生物作为针对VEGFR-2的双抗癌抗氧化剂

Fatma AlZahraa A A Mohamed¹, Dagmara Kłopotowska², Mohammed K Abd El-Gaber³

¹Medicinal Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt.

Bioorganic chemistry

|October 24, 2025

概括

新的西醇衍生物显示出双重抗癌和抗氧化特性. 化合物5b表现出强烈的抗增殖和抗氧化作用,而化合物6b抑制了VEGFR-2,表现优于sorafenib.

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.
分子生物学分子生物学

背景情况:

索衍生物正在研究它们的治疗潜力.
向血管内皮生长因子受体2 (VEGFR-2) 是癌症治疗的一个关键策略.
开发具有双重抗癌和抗氧化活性的药物是可取的.

研究的目的:

合成和表征基于佐的新型二氧化碳化物和希夫基.
评估这些化合物的体外双重抗癌和抗氧化活性.
为了确定具有抗增殖作用的强效和选择性VEGFR-2抑制剂.

主要方法:

西醇衍生物的合成和表征 (thiosemicarbazides 5a-5d,希夫基6a-6r).
在体外对抗A-498和HepG2细胞系的抗增殖活性的评估.
使用DPPH清理方法评估抗氧化剂活性.
VEGFR-2抑制测定和分子建模研究 (分子动力学,DFT计算).

主要成果:

化合物5b和6b对A-498和HepG2细胞系表现出显著的抗增殖活性.
化合物5b显示出强烈的抗氧化活性 (IC50 = 11.17μM) 和诱导细胞循环停止.
化合物6b表现出强大的VEGFR-2抑制 (IC50 = 0.21μM),优于索拉芬尼.
化合物5a和5b显示有希望的诱导caspases3,7和9,表明apoptotic活动.

结论:

新型索衍生物具有显著的双重抗癌和抗氧化潜力.
化合物5b和6b被确定为进一步开发作为向VEGFR-2的抗癌剂的有希望的候选物质.
这项研究提供了关于VEGFR-2抑制和抗增殖效应的结构-活性关系的见解.

关键词:

血管新生的产生.佐提亚 (Benzothiazole) 是一种一种癌症癌症癌症癌症卡斯帕塞斯 (Caspase) 是一个分子建模分子建模在VEGFR-2的基础上,

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