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Design, synthesis and anti-tumor activity of oleanolic acid derivatives targeting EGFR
Yan-Qiu Meng1, Li-Ming Liu1, Dong-Ping Xu1
1Department of Chemical Engineering, Shenyang University of Chemical Technology, Shenyang, 110142, China.
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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