作为潜在抗癌剂的阿洛哌啶衍生物的设计、合成和生物学评价。

IF 1.3 3区医学 Q3 CHEMISTRY, APPLIED Journal of Asian Natural Products Research Pub Date : 2024-06-21 DOI:10.1080/10286020.2024.2349660

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引用次数: 0

摘要

对阿洛哌啶分子的不同位置进行了修饰，以提高其抗癌活性并开发抗癌药物。对 44 个合成化合物的体外抗癌活性进行了评估。讨论了修饰位置对抗癌活性的影响，并建立了结构-活性关系分析。在 N12 位置进行修饰的一系列新型化合物显示出比阿洛哌啶更强的细胞毒性。其中，化合物 22 对 PC9 细胞具有良好的体外抗癌活性，中位抑制浓度（IC50）为 1.43 μM。机理研究表明，化合物 22 能诱导 PC9 细胞凋亡和细胞周期停滞。这些结果证明了阿洛哌嗪硫脲衍生物在抗癌活性方面的潜力。

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Design, synthesis and biological evaluation of aloperine derivatives as potential anticancer agents

Modifications at different positions on the aloperine molecule were performed to improve its anticancer activity and develop anticancer drugs. The in vitro anticancer activities of 44 synthesized compounds were evaluated. The effect of modification positions on anticancer activity was discussed and a structure–activity relationship analysis was established. A novel series of compounds with modifications at the N12 position showed much higher cytotoxicity than aloperine. Among them, compound 22 displayed promising in vitro anticancer activity against PC9 cells with a median inhibitory concentration (IC₅₀) of 1.43 μM. The mechanism studies indicated that compound 22 induced cell apoptosis and cell cycle arrest in PC9 cells. These results demonstrate the potential of aloperine thiourea derivatives in anticancer activity.

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来源期刊

Journal of Asian Natural Products Research 医学-药学

CiteScore

3.20

自引率

5.90%

发文量

审稿时长

2.3 months

期刊介绍： The Journal of Asian Natural Products Research (JANPR) publishes chemical and pharmaceutical studies in the English language in the field of natural product research on Asian ethnic medicine. The journal publishes work from scientists in Asian countries, e.g. China, Japan, Korea and India, including contributions from other countries concerning natural products of Asia. The journal is chemistry-orientated. Major fields covered are: isolation and structural elucidation of natural constituents (including those for non-medical uses), synthesis and transformation (including biosynthesis and biotransformation) of natural products, pharmacognosy, and allied topics. Biological evaluation of crude extracts are acceptable only as supporting data for pure isolates with well-characterized structures. All published research articles in this journal have undergone rigorous peer review, based on initial editor screening and anonymized refereeing by at least two expert referees.