相关实验视频

Updated: Jun 15, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay

Published on: February 9, 2021

合成新型pyrazole乙的andrographolide和isoandrographolide作为强大的抗癌药物

Siva Kumar Rokkam¹, Manohar Bhujel¹, Dolly Jain²

¹Department of Chemistry, Sri Sathya Sai Institute of Higher Learning, Prasanthi Nilayam Andhra Pradesh India gnageswararao@sssihl.edu.in.

|August 23, 2024

概括

新型安德罗格拉福利德衍生物与皮拉部分显示强烈的抗癌活性. 化合物1g通过通过高反应性氧物种 (ROS) 诱导亡,有效地抑制了结肠癌细胞.

科学领域:

自然产品化学自然产品化学
药用化学医学化学
癌症研究癌症研究

背景情况:

癌症是全球主要的死亡原因,合成药物通常会引起不良影响.
天然产品,如andrographolide衍生物,由于副作用较少,提供了一个有希望的替代品.
安德罗格拉福利德及其衍生物因其显著的抗癌潜力而得到认可.

研究的目的:

为了合成新型3,19-(NH-3-aryl-pyrazole) 乙烯酸的andrographolide和isoandrographolide.
为了评估这些合成化合物的抗癌活性与人类癌症细胞系的小组对比.
研究强效抗癌衍生物的作用机制和结构-活性关系.

主要方法:

合成十六种新型的安德罗格拉福利德和异安德罗格拉福利德乙烯酸.
使用光谱技术进行表征 (H NMR,C NMR,HRMS,FT-IR,UV-vis).
对60个人类癌细胞系进行抗癌查 (NCI,美国),随后进行体外研究,包括细胞周期分析,细胞亡试验 (annexin V-FITC/PI) 和反应性氧物种 (ROS) 试验.
在 silico ADMET 和 Lipinski 特性评估.

主要成果:

四种合成的化合物在所有60个癌症细胞系中显示出有前途的50%增长抑制 (GI₅₀) 活性.
化合物1g显示出最强大的活性,IC₅₀为3.08μM,对HCT-116结肠癌细胞.
化合物1g诱导HCT-116细胞的亡,主要是通过细胞内ROS水平升高.
结构-活性关系研究表明,pyrazole部分对于抗癌性质至关重要.

结论:

新型安德罗格拉福利德乙,特别是那些包含皮拉部分的,具有显著的抗癌潜力.
化合物1g代表了结肠癌治疗的有前途的化合物,通过ROS介导的亡作用.
合成的化合物需要进一步研究,作为潜在的抗癌药物候选者.

更多相关视频

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines

Published on: June 23, 2019

Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions

Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions

Published on: July 17, 2020

相关概念视频

Preparation of 1° Amines: Gabriel Synthesis

Preparation of 1° Amines: Gabriel Synthesis

Direct alkylation is not a suitable method for synthesizing amines because it produces polyalkylated products. Gabriel synthesis is the most preferred method to exclusively make primary amines. The method uses phthalimide, which contains a protected form of nitrogen that participates in alkylation only once to predominantly give primary amines.
Strong bases like NaOH or KOH deprotonate the phthalimide to form the corresponding anion, which acts as a nucleophile. Further, the anion attacks an...

Aryldiazonium Salts to Azo Dyes: Diazo Coupling

Aryldiazonium Salts to Azo Dyes: Diazo Coupling

The reaction of weakly electrophilic aryldiazonium (also called arenediazonium) salts with highly activated aromatic compounds leads to the formation of products with an —N=N— link, called an azo linkage. This reaction, presented in Figure 1, is known as diazo coupling and occurs without the loss of the nitrogen atoms of the aryldiazonium salt. Highly activated aromatic compounds such as phenols or arylamines favor the diazo coupling reaction. The coupling generally occurs at the...

Cancer Therapies

Cancer Therapies

Cancer therapies are various modes of treatment, such as surgery, radiation therapy, and chemotherapy that are administered to cancer patients.
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...