Design, synthesis and anti-tumor activity of oleanolic acid derivatives targeting EGFR.

IF 1.3 3区医学 Q3 CHEMISTRY, APPLIED

Journal of Asian Natural Products Research Pub Date : 2025-06-18 DOI:10.1080/10286020.2025.2515260

Yan-Qiu Meng, Li-Ming Liu, Dong-Ping Xu, Guo Chen, Tong-Tong Gu

引用次数: 0

Abstract

With computer-aided drug design (CADD) technology, a total of 12 inhibitors of EGFR based on oleanolic acid (OA) derivatives were designed and synthesized with modification at C-3 and C-28 positions of OA. Their structures were confirmed by ¹H-NMR,¹³C-NMR and ESI-MS. The anti-tumor activities of these novel analogues were evaluated by MTT assay, and the results showed that the derivatives I₆ and II₂ had stronger cytotoxicity on A549 and MCF-7 cancer cells, which may be potential candidate compounds for tumor therapy.

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靶向EGFR齐墩果酸衍生物的设计、合成及抗肿瘤活性研究。

采用计算机辅助药物设计（CADD）技术，在齐墩果酸（OA）衍生物的C-3和C-28位点进行修饰，设计合成了12种EGFR抑制剂。它们的结构经1H-NMR、13C-NMR和ESI-MS确证。MTT法测定了这些新型类似物的抗肿瘤活性，结果表明其衍生物I6和II2对A549和MCF-7癌细胞具有较强的细胞毒性，可能是潜在的肿瘤治疗候选化合物。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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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.