In the present work, we describe the synthesis and characterization of five new versatile acyclic or macrocyclic ligands containing binaphtyl-linked pyridine, bipyridine, or phenanthroline groups in their framework (see Schemes 1-4). The structures of the ligands were elucidated on the basis of elemental analyses. 1R, (1)H-NMR, (13)C-NMR, and FAB mass spectra. The cytotoxicity of these compounds was tested in vitro by using the tetrazolium salt reduction (MTT) assay on A549 (human lung carcinoma epithelial like) cells. All Of the tested compounds induced time- and concentration-dependent cytotoxic effect.