Novel efficient anticancer agents and DNA-intercalators of 1,2,3-triazol-1,8-naphthalimides: design, synthesis, and biological activity

Two novel series of 3-1,2,3-triazol-1,8-naphthalimides 5a–e, 7a–e were synthesized easily by employing ‘click reaction’. Their bioactivities were evaluated. Compounds 5a–e were found to be more toxic against MCF-7 cells while 7a–e were more potent against 7721 cells, in particular 7a, the IC50 value of which against cell lines of MCF-7 and 7721 was 0.348 μM and 0.258 μM, respectively. Due to the phenyl group linked to 1,2,3-triazole, compound 5a not only showed higher DNA affinity but also more efficient DNA damaging ability than compound 7a.