5-Ethynylarylnaphthalimides as antitumor agents: Synthesis and biological evaluation.

@article{QuintanaEspinoza20175Ethynylarylnaphthalimide,
  title={5-Ethynylarylnaphthalimides as antitumor agents: Synthesis and biological evaluation.},
  author={P. Quintana-Espinoza and Pedro Mart{\'i}n-Acosta and {\'A}ngel Amesty and P. Mart{\'i}n-Rodr{\'i}guez and I. Lorenzo-Castrillejo and L. Fern{\'a}ndez-P{\'e}rez and F. Mach{\'i}n and A. Est{\'e}vez-Braun},
  journal={Bioorganic \& medicinal chemistry},
  year={2017},
  volume={25 6},
  pages={
          1976-1983
        }
}
A set of 5-ethynylarylnaphthalimides was synthesized by Sonogashira cross-coupling reactions and evaluated for antiproliferative and antitopoisomerase II in vitro activities. Furthermore docking studies of these molecules as DNA-intercalators were carried out and the in vivo DNA-damaging activity was also determined with the model organism Saccharomyces cerevisiae. From the obtained results three naphthalimides 6, 13 and 14 showed strong topoisomerase II inhibitory activity. These three… Expand
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References

SHOWING 1-10 OF 28 REFERENCES
Synthesis, structural, and biological evaluation of bis-heteroarylmaleimides and bis-heterofused imides.
...
1
2
3
...