Metallo-organic complexes of copper(II) have established their recognition in bioinorganic chemistry due to the several in vitro & in vivo activities and reflected their worth in medicinal field during the studies and in treatment of considerable number of serious ailments. In many bio-systems, plenty information is available to exhibit their biochemical properties and route of function in numerous biological schemes, blended with novel prospects furnished by the blooming technologies of clinical field, is paving an exciting consequence for the expansion of an unusual group of vastly active medicine with curtailed side effects that could enhance considerably the present medical exploration. We are making herewith a sincere endeavour to document all the literature concerned in an appropriate chronology.