Artificial Zinc(II) Complexes Regulate Cell Cycle and Apoptosis‐Related Genes in Tumor Cell Lines

Abstract

Various proteins involved in transcriptional regulation possess highly selective DNA‐binding domains, known as zinc fingers. However, little is known about small‐molecule zinc(II) complexes in the regulation of gene expression and programmed cell death. A new family of zinc(II) complexes is reported, which might be useful against human cancer cells. By using template synthesis and in vitro cell‐line screening, a set of zinc(II) complexes has been found to induce apoptosis of cancer cells and display single‐reagent in vitro cytotoxicity. The method used to synthesize the molecules resulted in “built‐in” luminescent behavior. Confocal optical imaging clearly demonstrated penetration through the cell membrane by these metal complexes. We have discovered that C3, the meso‐zinc(II) complex is an extremely efficient regulator of the cell cycle and anti‐apoptosis genes bcl‐2 and bcl‐xL. This study provides a new insight into the development of zinc(II) complexes as potential drugs.