The interactions between K[PtCl3(C2H4)].H2O (Zeise salt) and three derivaties of bipyridinketone including bis(2-pyridyl)keton (BpyK), bis(2-pyridyl)-dibromoethene (BpyBE) and bis(2-pyridyl)-di(4-methoxyphenyl)ethene (BpyPhE) have been investigated for the first time. The results show that in the different reaction conditions, BpyK readily replaces the clhrorido ligand in trans position to the ethylene in Zeise to form complex trans-[PtCl2(C2H4)(BpyK)] (P1) with high yield of 85%. Mean while, the ethylen and the chlrorido ligand in cis position to it in Zeise are readily replaced by both BpyBE and BpyPhE to produce chellating complexes cis-[PtCl2(BpyBE)] (P2) and cis-[PtCl2(BpyPhE)] (P3) in very high yields (95%), respectively. The structures of P1−P3 were determined by Pt percentage, IR, UV-Vis, ESI-MS, 1H NMR spectroscopy, and also by 13C NMR spectroscopy for P3. The result of testing in vitro cytotoxicity of complex P2 and P3 against KB and Hep G2 human cancer cell lines indicates that complex P3 exhibits much better activity than P2. P3 also shows greater activity against Hep-G2 cell line in comparison to cisplatin with IC50 value of 6.78 μM.