A series of novel cisplatin-type platinum complexes, formulated as [PtA2(OCOCH2OR)2] (A2 = two monoamines or one diamine, R is an alkyl group), were designed, characteristic of alkoxyacetate as carboxylato ligands. The pertinent compounds were prepared and characterized by elementary analyses, IR, 1H NMR, and ESI-MS spectra. The cytotoxic activities of compound 1a in vitro toward HL-60 human leukemia and BEL-7402 human hepatocellular carcinoma cell lines were pioneeringly studied. Then, compounds 1b-3d were evaluated for their in vitro cytotoxicity against Ramos human lymphoma, 3AO human ovarian carcinoma, and A549 human non-small cell lung cancer cell lines. Most of them showed better cytotoxic activity than carboplatin against above selected cell lines.