Design, synthesis and anti-tumor activity of oleanolic acid derivatives targeting EGFR
With computer-aided drug design (CADD) technology, a total of 12 inhibitors of EGFR based on oleanolic acid (<b>OA</b>) derivatives were designed and synthesized with modification at C-3 and C-28 positions of <b>OA</b>. Their structures were confirmed by <sup>1</sup>H-NMR,<sup>13</sup>C-NMR and ESI-MS. The anti-tumor activities of these novel analogues were evaluated by MTT assay, and the results showed that the derivatives <b>I<sub>6</sub></b> and <b>II<sub>2</sub></b> had stronger cytotoxicity on A549 and MCF-7 cancer cells, which may be potential candidate compounds for tumor therapy.
Authors
- Tong‐Tong Gu
- Li Liu (ORCID: https://orcid.org/0000-0003-3022-936X)
- Yanqiu Meng
- Dongping Xu (ORCID: https://orcid.org/0000-0002-0754-4620)
- Guo Chen (ORCID: https://orcid.org/0000-0002-5200-5802)
Institutions
- Shenyang University of Chemical Technology (CN)
Publication Details
- Journal
- Journal of Asian Natural Products Research
- Published
- 2025-06-18
- DOI
- https://doi.org/10.1080/10286020.2025.2515260
- Primary Topic
- Natural product bioactivities and synthesis
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- National Natural Science Foundation of China