设计,合成和生物评估新的潜在的不寻常的修饰抗癌免疫调节剂,用于可能的非致病性基纳佐林基塔利多米德类似物
Reda R Mabrouk1,2, Abdallah E Abdallah1, Hazem A Mahdy1
1Pharmaceutical Medicinal Chemistry & Drug Design Department, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo 11884, Egypt.
International journal of molecular sciences
|August 12, 2023
概括
16种新的thalidomide类似物显示出对肝,前列腺和乳腺癌细胞的强有力的抗癌活性. 化合物XIIIa和XIVc显示出作为癌症治疗新药候选药物的巨大潜力.
科学领域:
- 药用化学 医学化学
- 在瘤学瘤学.
- 药理学 药理学是指药理学的学科.
背景情况:
- thalidomide类似物正在研究抗癌性质.
- 现有的癌症疗法需要具有提高疗效的新药候选药物.
研究的目的:
- 为了合成和评估新型的thalidomide类似物对抗繁殖活性.
- 为了确定强大的抗癌剂用于进一步的药物开发.
主要方法:
- 合成了16种新的thalidomide类似物.
- 针对HepG-2,PC3和MCF-7癌细胞系的体外抗增殖试验.
- 对IC50值,NFκB P65,caspase-8,TNF-α和VEGF水平进行分析.
主要成果:
- 几种类似物体在体外表现出强烈的抗增殖活性,表现优于thalidomide.
- 化合物XIIIa在经过测试的细胞系中显示出具有较低IC50值的最高功效.
- 化合物XIVc显著降低了NFκB P65,增加了caspase-8,降低了TNF-α和VEGF水平,诱导了细胞亡和细胞循环停止.
结论:
- 合成的thalidomide类似物,特别是XIIIa和XIVc,是有希望的抗癌候选物.
- 为了开发新的抗癌药物,需要对这些化合物的进一步评估.
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