Effects on Human Non-Small Lung Cancer Cell growth of Cu(II), Au(III) and Re(I) Complexes Containing N-donor Pyridyl Ligands

Hands-on synthetic laboratory experiences are critically important for undergraduate chemistry majors. A senior undergraduate research experience at the College of Wooster is presented in the current work. The inorganic complexes [Cu(phenan)2(NO3)2 ] (1; phenan = phenanthridine) and [Au(phenan)Cl3](2) were prepared by metallation of the phenan ligand in a 1:1 CH3OH/CH2 Cl2 mixture at room temperature. Complex 1 is a new inorganic coordination compound. The structures were confirmed by X-ray crystallography. Complex 1 reveals a distorted octahedral geometry around the central Cu (II) metal ion. In complex 2 , the Au(III) atom exhibits a square planar geometry. In addition, we investigated [Cu(dmeobpy)(H2O)2][NO3]2 (3; dmeobpy = 4,4’-dimethoxy-2,2’-bipyridine), [Cu(bap)(NO3)2](4; bap = 2,6-bis(azaindole)pyridine) and [Re(CO)3(dmeobpy)Cl] (5). The cytoxocities of 1-5, phenan, dmeobpy, bap and cisplatin were evaluated against several human non-small cell lung cancer cell lines (NCI-H1975, HCC827, NCI-H460, and NCI-A549). Compound 1 exhibited modest antitumor activity against the HCC827 cell line, with an IC 50 value of 19 µM. Compound 3 exhibits lower cytotoxic activity than 1 . The cytotoxic activity of complex 5 ( IC50<11 µM) is significantly greater than 1 and 3 against the H1975 cancer cell line.