Methylglycine, also known sarcosine, is dramatically used in drug molecules and its metal complexes can interact to DNA and also do cleavage. Hence, to study the influence of methylglycine ligand on biological behavior of metal complexes, two water-soluble platinum (II) complexes with the formula cis-[Pt(NH3)(2)(CH3-gly)]NO3 and cis-[Pt(NH2-CH3)(2)(CH3-gly)]NO3 (where CH3-gly is methylglycine) have been synthesized and characterized by spectroscopic methods, molar conductivity measurements, and elemental analyzes. The anticancer activity of synthesized complexes was tested against human breast adenocarcinoma cell line of MCF7 using MTT assay and results showed excellent anticancer activity with Cc(50) values of 126 and 292M after 24h incubation time, for both complexes of cis-[Pt(NH3)(2)(CH(3)gly)]NO3 and cis-[Pt(NH2-CH3)(2)(CH(3)gly)]NO3, respectively. Also, the interaction between Pt(II) complexes with calf thymus DNA was extensively studied by means of absorption spectroscopy, fluorescence titration spectra displacement with ethidium bromide (EtBr), and circular dichroism studied in Tris-buffer. The obtained spectroscopic results revealed that two complexes can bind to highly polymerized calf thymus DNA cooperatively and denature at micromolar concentrations. The fluorescence data indicate that quenching effect for cis-[Pt(NH3)(2)(CH(3)gly)]NO3 (K-sv=9.48mM(-1)) was higher than that of cis-[Pt(NH2-CH3)(2)(CH(3)gly)]NO3 (K(sv=)1.98mM(-1)). These results were also confirmed by circular dichrosim spectra. Consequently, docking data showed that cis-[Pt(NH3)(2)(CH(3)gly)]NO3 with more interaction energy binds on DNA via groove binding which is more compatible with experimental results.Two anticancer Pt(II) complexes, cis-[Pt(NH3)(2)(CH(3)gly)]NO3 and cis-[Pt(NH2-CH3)(2)(CH(3)gly)]NO3, have been synthesized and interacted with calf thymus DNA. Improving solubility of these compounds reduce side effects and increase anticancer activity against human breast cell line. Modes of binding have been studied by electronic absorption, fluorescence, and CD measurements. Results show that both Pt(II) complexes can interact to DNA via groove binding.which is more compatible with experimental results.