当前位置: X-MOL 学术Bioorg. Med. Chem. Lett. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Design of Antitumor Agents Containing Carbohydrate Based on GLUT1, and Evaluation of Antiproliferative Activity
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2017-04-02 05:01:36
Renshuai Zhang, Lairong Song, Bo Jiang, Lijun Wang, Ning Wu, Shuju Guo, Dayong Shi

A series of novel carbohydrate-modified antitumor compounds were designed based on glucose transporter 1 (GLUT1), and evaluated for their anticancer activities against four cancer cell lines. The ribose derivatives (compound 9 and 10) exhibited modest inhibitory activity. The compound 9 significantly inhibited the migration of A549 cell and induced A549 cell apoptosis in a concentration-dependent manner. Moreover, compound 9 blocked A549 cells at the G0/G1 phase. The cellular uptake studies suggested that ribose-modified compound 9 could be taken through GLUT1 in A549 cell line.

中文翻译:

基于GLUT1的含糖抗肿瘤药的设计及抗增殖活性的评价

基于葡萄糖转运蛋白1(GLUT1)设计了一系列新型的碳水化合物修饰的抗肿瘤化合物,并评估了它们对四种癌细胞系的抗癌活性。核糖衍生物(化合物9和10)表现出适度的抑制活性。化合物9以浓度依赖性方式显着抑制A549细胞的迁移并诱导A549细胞凋亡。此外,化合物9在G0 / G1期阻断了A549细胞。细胞摄取研究表明,核糖修饰的化合物9可以通过GLUT1在A549细胞系中摄取。
更新日期:2017-04-02
down
wechat
bug