Premium
Design, Synthesis, and In Vitro Anti‐Tumor Activities of 1,2,3‐triazole‐tetraethylene Glycol Tethered Heteronuclear Bis‐Schiff Base Derivatives of Isatin
Author(s) -
Wang Ruo,
Yin Xueyang,
Zhang Yaohuan,
Zhang Tesen,
Shi Weixiong
Publication year - 2018
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3341
Subject(s) - hela , chemistry , isatin , heteronuclear molecule , schiff base , in vitro , etoposide , triazole , stereochemistry , combinatorial chemistry , biochemistry , organic chemistry , nuclear magnetic resonance spectroscopy , medicine , surgery , chemotherapy
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 IC 50 in a range of 9.79–48.75 μM and were more potent than etoposide against Hela, HCT‐116, and A549 cell lines. In particular, the most potent bis‐Schiff base 9g (IC 50 : 9.79–29.64 μg/mL) was highly active against the five cancer cell lines tested, could act as a lead for further optimization.