细胞毒性
紫杉醇
吉非替尼
化学
MTT法
肿瘤细胞
体外
立体化学
药理学
癌症
生物化学
传统医学
生物
癌症研究
医学
受体
表皮生长因子受体
遗传学
作者
Meng Yang,Zhiqi Wang,Jinming Li,Da Xu,Bei-Bei Meng,Mei-Qi Huang
标识
DOI:10.1080/10286020.2023.2202855
摘要
To discovery novel VEGFR inhibitors, 12 novel asiatic acid derivatives were designed by computer-aided drug design (CADD) technology. Then, these novel asiatic acid derivatives were synthesized by introducing active groups at ring A and C-28 positions of asiatic acid. The structures of these novel analogues were confirmed by NMR and MS. Moreover, the anti-tumor activities of these novel asiatic acid derivatives on human hepatoma cells HepG2 and human gastric cancer cells SGC7901 were evaluated by MTT assay. As a result, compounds I2 and II4 showed stronger cytotoxicity on tumor cells than asiatic acid and positive control drugs such as gefitinib and paclitaxel. In conclusion, our study synthesized twelve novel asiatic acid derivatives and determined compounds I2 and II4 had better anti-tumor effect which may be potential candidate compounds for tumor therapy.
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