化学
体内
细胞培养
立体化学
药理学
结构-活动关系
药代动力学
癌细胞系
化学合成
体外
组合化学
癌症
生物化学
癌细胞
内科学
医学
遗传学
生物技术
生物
作者
Mingyue Zheng,Cheng-Hui Xu,Jingyu Ma,Yan Sun,Feifei Du,Hong Liu,Liping Lin,Chuan Li,Jian Ding,Kaixian Chen,Hualiang Jiang
标识
DOI:10.1016/j.bmc.2006.11.028
摘要
A series of triaminotriazine derivatives (compounds 5a–f, 6a–x, and 7a–g) was designed, synthesized, and evaluated for their inhibition activities to colorectal cancer (CRC) cell lines (HCT-116 and HT-29). Most of the synthesized compounds demonstrated moderate anti-proliferatory effects on both HCT-116 and HT-29 cell lines at the concentration of 10 μM. The inhibitory activities against HCT-116 and HT-29 cell lines were discussed to develop the structure–activity relationships of this new series. Compounds 6l and 6o exhibited prominent inhibition activities toward HCT-116, with IC50s of 0.76 and 0.92 μM, respectively. The in vivo antitumor studies and pharmacokinetics of compound 6l showed that it might be a promising new hit for further development of antitumor agents.
科研通智能强力驱动
Strongly Powered by AbleSci AI