Structure-based design and evaluation of naphthalene diimide G-quadruplex ligands as telomere targeting agents in pancreatic cancer cells.

@article{Micco2013StructurebasedDA,
  title={Structure-based design and evaluation of naphthalene diimide G-quadruplex ligands as telomere targeting agents in pancreatic cancer cells.},
  author={Marialuisa Micco and Gavin W Collie and Aaron G. Dale and Stephan A. Ohnmacht and Ingrida Pazitna and Mekala Gunaratnam and Anthony P. Reszka and Stephen Neidle},
  journal={Journal of medicinal chemistry},
  year={2013},
  volume={56 7},
  pages={2959-74}
}
Tetra-substituted naphthalene diimide (ND) derivatives with positively charged termini are potent stabilizers of human telomeric and gene promoter DNA quadruplexes and inhibit the growth of human cancer cells in vitro and in vivo. The present study reports the enhancement of the pharmacological properties of earlier ND compounds using structure-based design. Crystal structures of three complexes with human telomeric intramolecular quadruplexes demonstrate that two of the four strongly basic N… CONTINUE READING
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