A series of Zn(II) complexes, [Zn(MTS)2(tmeda)] (1), [Zn(MTS)2(2,2-bipy.)] (2), [Zn(MTS)2(1,10-phen.)] (3) and [Zn(MTS)2(4,4-bipy.)2]n (4), (where MTS = methylthiosalicylate, and tmeda = tetramethyl ethylenediamine, bipy.= bipyridyl, phen=phenanthroline ), have been synthesized and characterized by single crystal X-ray analysis and other spectroscopic techniques. The geometry of complex 3 is distorted square pyramidal around the Zn center, while complex 2 has distorted trigonal bipyramidal geometry. Complexes 1 and 4 show distorted tetrahedral geometry in which complex 4 has a zig-zag polymeric structure. Due to differences in geometries, these Zn complexes are expected to exhibit differences in their biological activities. We have carried out studies on DNA and protein binding, anticancer activity as well as cytotoxicity of these complexes. The anticancer activities were cell-line dependent, however, the complex 4 was found to be most active.