恶唑
化学
立体化学
康布雷他汀
咪唑
戒指(化学)
秋水仙碱
微管蛋白
铅化合物
化学合成
部分
细胞毒性
生物活性
IC50型
组合化学
效力
体外
微管
生物化学
医学
内科学
有机化学
生物
细胞生物学
作者
Jie Zhou,Jing Jin,Yi Zhang,Yuwen Yin,Xiaoguang Chen,Bo Xu
标识
DOI:10.1016/j.ejmech.2013.08.006
摘要
A series of novel oxazole-bridged analogs of combretastatin A-4 bearing a benzo[d]-imidazole as B ring were synthesized and evaluated for antiproliferative activities against five human cancer cell lines. Among all the synthesized compounds, the N-unsubstituted benzoimidazole analog 5 and the analogs 6b, 7a and 7b with a small hydrophobic group on nitrogen atom of benzoimidazole ring were identified as the most potent inhibitors of tumor cell growth with IC50 values at nanomolar levels (5, IC50 = 8.4 nM, HT29; 6b, 7a, 7b, IC50 = 9.6 nM, 3.8 nM, 3.0 nM, A549). In a murine H22 tumor xenograft model, compound 5 exhibited significant antitumor activity. The binding mode of compound 5 in the colchicine binding site of tubulin was probed.
科研通智能强力驱动
Strongly Powered by AbleSci AI