三碳烯 (Tricarbonyl rhenium) 复合物与8-基诺林:具有结构性,化学性,抗菌性和抗癌性
Krzysztof Łyczko1, Anna Pogorzelska2, Urszula Częścik2
1Institute of Nuclear Chemistry and Technology Dorodna 16 03-195 Warsaw Poland k.lyczko@ichtj.waw.pl j.rode@ichtj.waw.pl.
RSC advances
|June 6, 2024
概括
合成并测试了12种新的三碳烯 () 复合物,以检测它们的生物活性. 一个复合物显示对Pseudomonas aeruginosa增强的抗菌作用,而几个化合物对癌症细胞系表现出选择性细胞毒性.
科学领域:
- 无机化学 无机化学 有机化学
- 协调化学 协调化学
- 药用化学 医学化学
背景情况:
- 三碳烯 (Tricarbonyl rhenium) 复合物为开发新型治疗剂提供了一个多功能支架.
- "2 + 1"协调系统允许通过将阳离子双酸N,O-捐赠体连接物与中性N-捐赠体隔离体结合起来进行模块化合成.
- 探索结构-活性关系对于识别强效和选择性生物活性化合物至关重要.
研究的目的:
- 合成和描述一系列12种新型三碳复合物.
- 评估合成的复合体对各种细菌菌株的抗菌活性.
- 评估复合体的细胞毒性和选择性,与人类癌症和非癌症细胞系的小组对比.
主要方法:
- 使用阳离子N,O-捐赠体 (8-基因衍生物) 和中性N-捐赠体二醇合成十二种三碳烯 () 复合物.
- 使用单晶X射线衍射 (scXRD) 的结构阐明和与密度函数理论 (DFT) 计算的比较.
- 通过元素分析 (EA),FT-IR,NMR和UV-Vis光谱学进行表征,得到DFT和时间依赖的DFT (TD-DFT) 计算的支持.
- 生物评估,包括针对格拉姆阴性和格拉姆阳性细菌的抗菌试验和针对HL-60,SKOV-3,PC-3和MCF-7细胞系的细胞毒性试验.
主要成果:
- 大多数合成的 (renium) 复合物表现出有限的抗菌活性.
- [Re(CO) 3(MeQ) Him]对*Pseudomonas aeruginosa*表现出显著的抗菌活性,其表现优于自由的MeHQ配体.
- 一些化合物,包括HQ,ClHQ配体和[Re(CO) 3(Q) Hdmpz]复合体,对MCF-7乳腺癌细胞系具有良好的选择性.
- 所有合成的复合物都对HL-60细胞表现出敏感性,IC50值在1.5至14μM之间,尽管纯HQ和ClHQ配体略有强大.
结论:
- 合成的三碳烯复合物表现出各种各样的生物特征.
- 复合物[Re(CO) 3[MeQ) Him]是作为抗菌剂进一步研究的有希望的候选物.
- 这项研究强调了这些复合体在选择性癌症治疗中的潜力,特别是针对HL-60细胞,并保证了对连接物修饰的进一步探索,以提高有效性和选择性.
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