吉非替尼
化学
紫杉醇
立体化学
体外
阳性对照
血管内皮生长因子受体
MTT法
碳-13核磁共振
活性化合物
肿瘤细胞
药理学
传统医学
癌症
生物化学
受体
生物
表皮生长因子受体
癌症研究
医学
遗传学
作者
Meng Yang,Yue-Jiao Wu,Zhen-Yu Kuai,Jun-Jiao Ma,Zan Wang,Bei-Bei Meng,Zhiqi Wang
标识
DOI:10.1080/10286020.2022.2093194
摘要
The VEGF receptor is mock-coupled with a known active compound and the active groups of the inhibitor which can bind to VEGF were analyzed. Using asiatic acid as a lead compound, 10 novel skeleton candidate compounds were designed through introduction of the active groups onto the special location and synthesized simultaneously. Furthermore, the structure of these compounds was determined by 1H NMR, 13C NMR and MS and 9 compounds were identified as the new compounds. Moreover, the in vitro anti-tumor activities of these new compounds were determined by MTT assay on two cancer cell lines (HepG2 and SGC-7901). The results showed that compounds I1 and II2 have more potent anticancer activity than positive control drugs such as gefitinib and paclitaxel.
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