Synthesis, characterization and in vitro antitumor activity of asiatic acid derivatives

IF 3.1 4区医学 Q3 CHEMISTRY, MEDICINAL

Medicinal Chemistry Research Pub Date : 2025-06-05 DOI:10.1007/s00044-025-03431-3

Panpan Wang, Jie Liu, Lantian Cui, Gao Li, Longxuan Zhao, Mei Jin

引用次数: 0

Abstract

Twenty-seven asiatic acid derivatives were designed and synthesized in this paper, including twenty-two new compounds. The synthesized compounds were confirmed by ¹H NMR, ¹³C NMR and HRMS. The antitumor activities of all compounds against A549, Hela and HepG2 cancer cells in vitro were evaluated. Notably, AA-6a (IC₅₀ = 1.10 ± 0.25 μM) has better antitumor activity than gefitinib (IC₅₀ = 83.75 ± 1.72 μM) against A549 cells. AA-6b (IC₅₀ = 2.38 ± 0.36 μM) has better antitumor activity than gefitinib (IC₅₀ = 33.88 ± 1.51 μM) on Hela cells. AA-2b (IC₅₀ = 1.55 ± 0.21 μM) has the better antitumor activity than gefitinib (IC₅₀ = 48.37 ± 1.07 μM) against HepG2 cells.

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积雪草酸衍生物的合成、表征及体外抗肿瘤活性研究

设计合成了27个亚细亚酸衍生物，其中22个为新化合物。合成的化合物经1H NMR、13C NMR和HRMS确证。研究了各化合物对A549、Hela和HepG2癌细胞的体外抗肿瘤活性。值得注意的是，AA-6a对A549细胞的抗肿瘤活性（IC50 = 1.10±0.25 μM）优于吉非替尼（IC50 = 83.75±1.72 μM）。AA-6b对Hela细胞的抗肿瘤活性（IC50 = 2.38±0.36 μM）优于吉非替尼（IC50 = 33.88±1.51 μM）。AA-2b对HepG2细胞的抗肿瘤活性（IC50 = 1.55±0.21 μM）优于吉非替尼（IC50 = 48.37±1.07 μM）。

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来源期刊

Medicinal Chemistry Research 医学-医药化学

CiteScore

4.70

自引率

3.80%

发文量

162

审稿时长

5.0 months

期刊介绍： Medicinal Chemistry Research (MCRE) publishes papers on a wide range of topics, favoring research with significant, new, and up-to-date information. Although the journal has a demanding peer review process, MCRE still boasts rapid publication, due in part, to the length of the submissions. The journal publishes significant research on various topics, many of which emphasize the structure-activity relationships of molecular biology.