替代的 ((I) 金属循环:一种新型强效抗癌剂
Reema L Borkar1, Chandra Lekha Putta2, Bhaskaran Shankar3
1School of Chemistry, University of Hyderabad, Hyderabad, 500 046, India.
Chemistry, an Asian journal
|April 14, 2025
概括
替代的 ((I) 金属环表现出强烈的抗癌活性,性能优于西斯,并突出了替代对抗癌细胞有效性的影响.
科学领域:
- 有机金属化学 有机金属化学
- 药用化学 医学化学
- 材料科学 材料科学 材料科学
背景情况:
- (I) 金属循环被探索用于治疗应用.
- 了解替代在生物活性中的作用至关重要.
研究的目的:
- 合成和描述新的和非替代的 (I) 金属环.
- 评估它们的体外抗癌活性和生物相容性.
- 研究最强效化合物的作用机制.
主要方法:
- 协调驱动的一溶解热合成.
- 使用元素分析,质谱,IR,NMR和PXRD进行表征.
- 单晶X射线衍射 (SCXRD) 用于结构的确定.
- 在体外细胞毒性测定对HeLa和B16癌细胞.
- 在L929和C2C12细胞系上进行生物相容性测试.
- 作用机制研究包括ROS生成,线粒体膜潜力,DNA结合和亡诱导.
- 用B-DNA进行分子对接研究.
主要成果:
- 成功合成了两个(I) 金属环,C1 (含) 和C2 (非含).
- 这两种化合物在体外对宫癌和皮肤癌细胞具有显著的抗癌活性,超过了西斯的抗癌活性.
- 与C2相比,用代替的C1表现出更高的抗癌效果,这表明具有显著的效果.
- C1诱导了细胞内ROS生成,破坏了线粒体膜潜能,与DNA结合,并在HeLa细胞中触发了亡.
- 分子对接揭示了与B-DNA的结合点和相互作用.
结论:
- 替代显著增强了这些 (I) 金属循环的抗癌作用.
- 金属环代表了抗癌药物开发的有希望的候选人.
- 观察到的活性归因于DNA损伤和亡诱导.
- 对这些化合物的进一步研究对于治疗应用是有必要的.
更多相关视频
10:52Line Shape Analysis of Dynamic NMR Spectra for Characterizing Coordination Sphere Rearrangements at a Chiral Rhenium Polyhydride Complex
Published on: July 27, 2022
2.6K
10:10Application of Elemental Lanthanides in the Selective C-F Activation of Trifluoromethylated Benzofulvenes Providing Access to Various Difluoroalkenes
Published on: July 28, 2018
6.4K
相关概念视频
Electrophilic Aromatic Substitution: Fluorination and Iodination of Benzene
5.7K
Bromination and chlorination of aromatic rings by electrophilic aromatic substitution reactions are easily achieved, but fluorination and iodination are difficult to achieve. Fluorine is so reactive that its reaction with benzene is difficult to control, resulting in poor yields of monofluoroaromatic products. To address this, Selectfluor reagent is used as a fluorine source in which a fluorine atom is bonded to a positively charged nitrogen.
5.7K
ortho–para-Directing Deactivators: Halogens
5.2K
Halogens are ortho–para directors. They are more electronegative than carbon. Therefore, as ring substituents, they can withdraw electrons through the inductive effect and deactivate the aromatic ring towards electrophilic substitution. Halogens also have an electron-donating resonance effect on the ring, which influences the orientation of the incoming electrophile. If an electrophile attacks at the ortho or the para position, the halogen donates electrons and stabilizes the intermediate...
5.2K
Mitogens and the Cell Cycle
6.3K
Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...
6.3K
Targeted Cancer Therapies
7.4K
The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
There are several types of targeted therapies against...
7.4K
