靶向VEGFR的水飞蓟宾衍生物的合成及抗肿瘤活性研究。

IF 1.3 3区医学 Q3 CHEMISTRY, APPLIED

Journal of Asian Natural Products Research Pub Date : 2025-06-18 DOI:10.1080/10286020.2025.2515250

Lei Gao, Liang-Feng Zhang, Yan Li, Chao-Hui Zhang, Yan-Qiu Meng

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引用次数: 0

摘要

通过酰化、选择性氨解、烷基化、氧化和脱氢等反应对水飞蓟宾C-3和C-7位羟基进行修饰，设计合成了10种基于水飞蓟宾衍生物的VEGFR抑制剂。经质谱、1H NMR和13C NMR确证了它们的结构。体外活性测定表明，这些化合物均能抑制A549和SGC7901细胞的增殖，特别是化合物I3和I8对这些肿瘤细胞的抑制活性较好，且与阳性对照药物拉帕替尼相似，可能是潜在的肿瘤治疗候选化合物。

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Synthesis and antitumor activity of silibinin derivatives targeting VEGFR.

Totally 10 inhibitors of VEGFR based on silibinin derivatives were designed and synthesized with the modification on the hydroxyl group at C-3 and C-7 positions of silibinin through acylation, selective aminolysis, alkylation, oxidation, and dehydrogenation reactions. Their structures were confirmed by MS, ¹H NMR, and ¹³C NMR. In vitro activity assay showed that these compounds can inhibit cell proliferation of A549 and SGC7901 cells, especially compounds I₃ and I₈ showed better inhibitory activity on these tumor cells, and similar to the positive control drug lapatinib, which may be potential candidate compounds for tumor therapy.

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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.