含氮杂环的 β-咔啉衍生物的设计、合成和生物活性评估。

IF 4.2 2区化学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Molecules Pub Date : 2024-10-31 DOI:10.3390/molecules29215155

Guiyun Wu, Wenhang Wang, Fulian Li, Chenlu Xu, Yue Zhou, Zhurui Li, Bingqian Liu, Lihui Shao, Danping Chen, Song Bai, Zhenchao Wang

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引用次数: 0

摘要

研究人员设计并合成了一系列含氮杂环的β-咔啉衍生物。筛选了所有化合物对四种人类肿瘤细胞系（A549、K562、PC-3、T47D）的抗肿瘤活性。值得注意的是，化合物 N-(4-(吗啉甲基)苯基)-2-((5-(1-(3,4,5-三甲氧基苯基)-9H-吡啶并[3,4-b]吲哚-3-基)-1,3,4-恶二唑-2-基)硫)乙酰胺（8q）对 PC-3 细胞具有显著的抑制活性，IC50 值为 9.86 µM。重要的是，化合物 8q 能有效抑制 PC-3 细胞的增殖和迁移。机理研究显示，化合物 8q 可诱导细胞凋亡，并引起活性氧（ROS）的积累，导致 PC-3 细胞的细胞周期停滞在 G0/G1 期。

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Design, Synthesis and Biological Activity Evaluation of β-Carboline Derivatives Containing Nitrogen Heterocycles.

A series of β-carboline derivatives containing nitrogen heterocycles were designed and synthesized. All compounds were screened for their antitumor activity against four human tumor cell lines (A549, K562, PC-3, T47D). Notably, compound N-(4-(morpholinomethyl)phenyl)-2-((5-(1-(3,4,5-trimethoxyphenyl)-9H-pyrido[3,4-b]indol-3-yl)-1,3,4-oxadiazol-2-yl)thio)acetamide (8q) exhibited significant inhibitory activity against PC-3 cells with an IC₅₀ value of 9.86 µM. Importantly, compound 8q effectively suppressed both the proliferation and migration of PC-3 cells. Mechanistic studies revealed that compound 8q induced cell apoptosis and caused the accumulation of reactive oxygen species (ROS), leading to cell cycle arrest in the G0/G1 phase in PC-3 cells.

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来源期刊

Molecules 化学-有机化学

CiteScore

7.40

自引率

8.70%

发文量

7524

审稿时长

1.4 months

期刊介绍： Molecules (ISSN 1420-3049, CODEN: MOLEFW) is an open access journal of synthetic organic chemistry and natural product chemistry. All articles are peer-reviewed and published continously upon acceptance. Molecules is published by MDPI, Basel, Switzerland. Our aim is to encourage chemists to publish as much as possible their experimental detail, particularly synthetic procedures and characterization information. There is no restriction on the length of the experimental section. In addition, availability of compound samples is published and considered as important information. Authors are encouraged to register or deposit their chemical samples through the non-profit international organization Molecular Diversity Preservation International (MDPI). Molecules has been launched in 1996 to preserve and exploit molecular diversity of both, chemical information and chemical substances.