Meng Yan-Qiu, Zhao Yu-Wei, Kuai Zhen-Yu, Liu Li-Wei, Li Wei
a Department of Pharmaceutical Engineering , Shenyang University of Chemical Technology , Shenyang 110142 , China.
J Asian Nat Prod Res. 2017 Oct;19(10):1000-1010. doi: 10.1080/10286020.2017.1283310. Epub 2017 Jan 31.
Ten novel oleanolic acid (OA) derivatives were synthesized through modifications at positions of A ring and C-28. Inhibitory activities of the oleanolic acid derivatives against SGC7901 and A549 cell lines were evaluated and confirmed by the tetrazolium bromidesalt (MTT) assay. The lab results revealed that all these compounds displayed some antitumor activity against SGC-7901 and A-549 cell lines. Among them, II and II exhibited excellent antitumor activities against SGC7901 cells and A549 cells, compared with gefitinib. Molecular docking studies have shown that compounds II and II produce potent antitumor activities by interacting with C-kit receptor through hydrogen bonds and hydrophobic bonds.
通过对A环和C-28位进行修饰，合成了10种新型齐墩果酸（OA）衍生物。采用四唑溴盐（MTT）法评估并确认了齐墩果酸衍生物对SGC7901和A549细胞系的抑制活性。实验结果表明，所有这些化合物对SGC-7901和A-549细胞系均表现出一定的抗肿瘤活性。其中，化合物II和III对SGC7901细胞和A549细胞表现出优异的抗肿瘤活性，与吉非替尼相当。分子对接研究表明，化合物II和III通过与C-kit受体形成氢键和疏水键相互作用，产生强效的抗肿瘤活性。
