Pt(II) complexes with a series of bifunctional bisphosphonate derivatives as ligands. Pt(II) complexes showed cytotoxicity and antiproliferative activity against MG-63. Synergistic effect on tumor cells by bisphosphonate moieties and dichloroplatinum skeleton. Typical complexes showed hydroxyapatite affinity superior to zoledronate and cisplatin. Representative compound induced apoptosis analogous to cisplatin.