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Solid-phase Synthesis of [4.4] Spirocyclic Oximes
Published on: February 6, 2019
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不对称的salen基氧化物VIV:合成,表征,生物分子相互作用和抗癌活性
Deepika Mohapatra1, Pratikshya Das Pattanayak1, Souvik Chatterjee2
1Department of Chemistry, National Institute of Technology, Rourkela, 769008, Odisha, India.
Journal of inorganic biochemistry
|December 29, 2024
概括
新的氧化 ((IV) 复合物与联体显示出显著的抗癌活性. 这些疏水性化合物有效地与生物分子相互作用,并诱导癌细胞的亡,复合体3是最强大的.
科学领域:
- 无机化学 无机化学
- 药用化学 医学化学
- 生物化学 生物化学
背景情况:
- 氧化瓦纳 (IV) 复合物正在探索治疗应用.
- 盐联体为金属复合体提供了多功能协调环境.
- 了解结构-活性关系对于药物开发至关重要.
研究的目的:
- 合成和描述新的氧化 ((IV) 复合物与不对称的联体.
- 评估这些复合物的稳定性,生物分子相互作用和体外抗癌特性.
- 研究其作用机制,包括诱导亡.
主要方法:
- 合成不对称的酸连接体 (H2L1-3) 和它们的氧化 (IV) 复合体 (1-3).
- 使用CHNS,IR,UV-Vis,NMR,HR-ESI-MS和单晶X射线衍射进行表征.
- 对HT-29,A549和NIH-3T3细胞系的溶液稳定性,DNA/BSA结合,分割系数和体外细胞毒性进行评估.
- 亡测定包括DAPI,AO/EB和双染色.
主要成果:
- 三种稳定的氧化 (IV) 复合物 (1-3) 已成功合成并进行结构特征.
- 复合物表现出良好的水稳定性和显著的生物分子相互作用 (DNA/BSA结合).
- 高水性表明有效的细胞膜透性.
- 复合体3对HT-29 (IC50 = 6.2 ± 0.2 μM) 和A549 (IC50 = 5.3 ± 0.4 μM) 细胞系表现出强烈的细胞毒性.
- 诱导亡通过各种测试得到证实.
结论:
- 合成的氧化 (IV) 复合物是稳定的,并与生物分子有效相互作用.
- 这些复合物,特别是复合物3,在体外表现出有前途的抗癌活性.
- 这些发现表明,有可能开发基于的新型抗癌剂.
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