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相关概念视频

Electron Transport Chain: Complex I and II01:46

Electron Transport Chain: Complex I and II

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The mitochondrial electron transport chain (ETC) is the main energy generation system in the eukaryotic cells. However, mitochondria also produce cytotoxic reactive oxygen species (ROS) due to the large electron flow during oxidative phosphorylation. While Complex I is one of the primary sources of superoxide radicals, ROS production by Complex II is uncommon and may only be observed in cancer cells with mutated complexes.
ROS generation is regulated and maintained at moderate levels necessary...
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Cycloaddition Reactions: Overview01:16

Cycloaddition Reactions: Overview

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Cycloadditions are one of the most valuable and effective synthesis routes to form cyclic compounds. These are concerted pericyclic reactions between two unsaturated compounds resulting in a cyclic product with two new σ bonds formed at the expense of π bonds. The [4 + 2] cycloaddition, known as the Diels–Alder reaction, is the most common. The other example is a [2 + 2] cycloaddition.
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Positive Regulator Molecules02:39

Positive Regulator Molecules

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Mitotic cell division results in daughter cells that exactly resemble the parent cell. However, errors in the DNA replication or distribution of genetic material may lead to genetic mutations that may be passed down to every new cell formed from the resulting abnormal cell. Propagation of such mutant cells is restricted through checkpoint mechanisms present at different stages of the cell cycle. These checkpoints involve regulator molecules that either promote or demote cell cycle events.
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Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

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The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
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Cycloaddition Reactions: MO Requirements for Thermal Activation01:16

Cycloaddition Reactions: MO Requirements for Thermal Activation

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Thermal cycloadditions are reactions where the source of activation energy needed to initiate the reaction is provided in the form of heat. A typical example of a thermally-allowed cycloaddition is the Diels–Alder reaction, which is a [4 + 2] cycloaddition. In contrast, a [2 + 2] cycloaddition is thermally forbidden.
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Pericyclic Reactions: Introduction01:17

Pericyclic Reactions: Introduction

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Pericyclic reactions are organic reactions that occur via a concerted mechanism without generating any intermediates. The reactions proceed through the movement of electrons in a closed loop to form a cyclic transition state, where rearrangement of the σ and π bonds yields specific products.
Pericyclic reactions can be classified into three categories: electrocyclic reactions, cycloaddition reactions, and sigmatropic rearrangements. Electrocyclic reactions and sigmatropic...
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Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
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利用Co (III) - 环二烯复合体开发抗癌剂

João Franco Machado1, Sandra Cordeiro2,3, Joana N Duarte1

  • 1Centro de Química Estrutural, Institute of Molecular Sciences, Faculdade de Ciências, Universidade de Lisboa, Campo Grande, 1749-016 Lisboa, Portugal.

Inorganic chemistry
|March 19, 2024
PubMed
概括
此摘要是机器生成的。

新的 (III) -cyclopentadienyl复合物通过诱导细胞死亡途径,对结直肠,卵巢和乳腺癌细胞系表现出强大的抗癌活性. 这些新型有机金属化合物显示出有前途的治疗潜力,没有观察到体内毒性.

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Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
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科学领域:

  • 有机金属化学 有机金属化学
  • 药用化学 医学化学
  • 癌症治疗方法 癌症治疗方法

背景情况:

  • 基于的药物在癌症治疗中面临局限性.
  • 有机金属复合物提供了替代治疗策略.
  • 半三明治有机金属复合物还没有得到充分的探索.

研究的目的:

  • 合成和描述新型的 (III) - cyclopentadienyl复合物.
  • 评估这些复合物的体外细胞毒性与各种人类癌症细胞系相比.
  • 调查体内毒性和作用机制.

主要方法:

  • 合成和完整的表征 (元素分析,光谱学,DFT).
  • 使用MTS试验进行体外细胞毒性评估 (HCT116,A2780,MDA-MB-231,MCF-7细胞系).
  • 在体内使用小胚胎黄囊膜 (YSM) 试验进行毒性评估.

主要成果:

  • 成功合成和特征化了四种新的 (III) - cyclopentadienyl复合物.
  • 对结直肠,卵巢和乳腺癌细胞系观察到高的体外细胞毒性.
  • 机制包括ROS产生,亡,自和线粒体膜破坏.
  • 在小胚胎YSM测定中没有检测到体内毒性.

结论:

  • 新型有机金属复合物具有显著的抗癌潜力.
  • 这些复杂物通过多种途径有效诱导癌细胞死亡.
  • 有望的无毒治疗候选人进行进一步的研究.