Cellular uptake and toxicity study of cis -bis(6-aminoquinoline) dichloroplatinum(II)

A fluorescent analog of cis -diamminedichloroplatinum(II), cis -bis(6-aminoquinoline)dichloroplatinum(II), was prepared from K 2 [PtCl 4 ] and 6-aminoquinoline (AQL). HPLC of the thiourea derivative of the new complex showed that it has the cis -configuration. The Pt-AQL complex and the parent ligand AQL were evaluated for biological activity and cellular uptake, using the ciliate Tetrahymena pigmentosa. The complex was relatively nontoxic at the tested levels below 5 × 10 −4 M, but did exhibit inhibition of culture growth at 5 × 10 −4 M. Measurement of cellular uptake of the Pt-AQL complex demonstrated incorporation into the cell, with localization primarily within the vacuoles of the cells. Comparable measurement of the parent ligand AQL showed little measurable cellular uptake.