Synthesis and initial in vitro biological evaluation of two new zinc-chelating compounds: comparison with TPEN and PAC-1.

@article{Strand2013SynthesisAI,
  title={Synthesis and initial in vitro biological evaluation of two new zinc-chelating compounds: comparison with TPEN and PAC-1.},
  author={O Alexander H Strand and Gulzeb Aziz and Sidra Farzand Ali and Ragnhild Elisabeth Paulsen and Trond V Hansen and P{\aa}l Rongved},
  journal={Bioorganic & medicinal chemistry},
  year={2013},
  volume={21 17},
  pages={5175-81}
}
The lipophilic, cell-penetrating zinc chelator N,N,N',N',-tetrakis(2-pyridylmethyl) ethylenediamine (TPEN, 1) and the zinc chelating procaspase-activating compound PAC-1 (2) both have been reported to induce apoptosis in various cell types. The relationship between apoptosis-inducing ability and zinc affinity (Kd), have been investigated with two new model compounds, ZnA-DPA (3) and ZnA-Pyr (4), and compared to that of TPEN and PAC-1. The zinc-chelating o-hydroxybenzylidene moiety in PAC-1 was… CONTINUE READING