立体/区域选择性获取替代的3-氧醇,并进行抗扩散评估和in silico验证
Preeti1, Asif Raza2, Amit Anand3
1Department of Chemistry, Guru Nanak Dev University Amritsar India vipan_org@yahoo.com.
RSC advances
|September 29, 2023
概括
研究人员开发了一个新的合成替代-3-基-2-oxindoles,显示强大的抗癌活性对结直肠癌,卵巢癌和黑色素瘤. 一种化合物在临床前模型中表现优于西斯.
科学领域:
- 药用化学 医学化学
- 有机合成 有机合成
- 癌症生物学 癌症生物学
背景情况:
- 3-基-2-氧醇是药物化学中一个特权的支架.
- 开发具有提高疗效和选择性的新型抗癌药物是一个至关重要的未满足的需求.
研究的目的:
- 开发一种立体/区域选择性合成路径,用于各种替代的-3-基-2-oxindoles.
- 评估这些新型化合物对各种癌症细胞系的抗增殖活性.
- 调查强效化合物的作用机制和目标接触.
主要方法:
- 立体/区域选择性合成替代的-3-基-2-oxindoles.
- 针对结直肠癌 (HCT116),卵巢癌 (OVCAR10) 和人类转移性黑色素瘤 (1205Lu) 细胞系的抗增殖试验.
- 用于结构特征的X射线衍射.
- 在体外卡斯帕酶介导的亡试验.
- 针对血管内皮生长因子受体2 (VEGFR2) 的分子对接研究.
主要成果:
- 一个被替代的-3-基-2-oxindoles的图书馆成功地合成了高立体和区域选择性.
- 一种合成的化合物显示出显著的抗增殖功效,超过西斯对HCT116,OVCAR10和1205Lu细胞系的1.2,2.12和1.55倍.
- 亡研究证实了该化合物诱导编程细胞死亡的能力.
- 分子对接揭示了与VEGFR2蛋白质的有利结合相互作用.
结论:
- 开发的合成方法提供了获得新型替代-3-基-2-oxindoles的机会.
- 强大的抗癌活性和有利的结合VEGFR2表明这些化合物是进一步药物开发的有希望的候选者.
- 这些发现需要进一步研究它们对各种癌症的治疗潜力.
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