优化光活性抗癌氧二-桥接二复合物的电子特性 (II,II)
Zhanyong Li1, Amanda David, Bryan A Albani
1Department of Chemistry, Texas A&M University , College Station, Texas 77840, United States.
Journal of the American Chemical Society
|December 2, 2014
概括
迪罗化合物与特定的皮里丁配体显示可调节的光反应性. 连接物修饰增强了光化疗的细胞毒性,诱导癌细胞的亡.
科学领域:
- 协调化学 协调化学
- 摄影化学的使用.
- 药用化学 医学化学
背景情况:
- 部分轮迪罗复合体因其独特的结构和反应性而引起人们的兴趣.
- 连接物替代剂对迪罗化合物的特性的影响尚未完全理解.
研究的目的:
- 为了合成和表征具有不同6-R-2-oxypyridine连接体的新型二化合物.
- 研究这些复合物的光化学和光动力学潜力.
- 为了将连接体结构与光反应性和细胞毒性相关联.
主要方法:
- 合成cis-[Rh2(xhp) 2(CH3CN) n][BF4]2复合体 (n=5或6),其中xhp = mhp, fhp, chp.
- 用于结构确定的X射线晶体学.
- 乙尼铁联体的溶液状态可变性研究.
- 光化学辐射实验以形成水中添加物.
- 对HeLa细胞系的细胞毒性测定.
- 细胞亡试验用于确定细胞死亡机制.
主要成果:
- 合成和结构性特征的迪罗复合体与 cis 导向的桥梁连接体.
- 确定了乙尼烯联结体可变性的顺序: -CH3 > -Cl > -F.
- 经过置复合物的辐射后,已证明增强了水中添加物形成 (5).
- 在辐射后观察到复合体5的细胞毒性显著增加 (16.4倍),而复合体7的毒性最小.
- 确认了细胞亡作为由复合体5诱导的细胞死亡机制.
结论:
- 在Dirhodium中心周围调整连接体场对于优化光反应性至关重要.
- 替代的迪罗复合物显示出有前途的光化疗潜力.
- 光反应性与增强的细胞毒性和光动力学作用直接相关.
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