Design, Synthesis, and In Vitro Anti-Tumor Activities of 1,2,3-triazole-tetraethylene Glycol Tethered Heteronuclear Bis-Schiff Base Derivatives of Isatin

作者:Wang, Ruo*; Yin, Xueyang; Zhang, Yaohuan; Zhang, Tesen; Shi, Weixiong
来源:Journal of Heterocyclic Chemistry, 2018, 55(12): 3001-3005.
DOI:10.1002/jhet.3341

摘要

We report herein the design, synthesis, and in vitro anti-tumor activities of a series of 1,2,3-triazole-tetraethylene glycol tethered heteronuclear bis-Schiff base derivatives of isatin. Our results indicated that all the synthesized bis-Schiff bases except 9e showed considerable in vitro anticancer activities against HepG2, Hela, HCT-116, A549, and MCF-7 human cancer cell lines with IC50 in a range of 9.79-48.75 mu M and were more potent than etoposide against Hela, HCT-116, and A549 cell lines. In particular, the most potent bis-Schiff base 9g (IC50: 9.79-29.64 mu g/mL) was highly active against the five cancer cell lines tested, could act as a lead for further optimization.