The organic salts can be serving as versatile building blocks for the synthesis of a number of important and often novel biologically active compounds. Some examples for the strategic use of amines transformations that enable efficient, flexible and straightforward synthesis of structurally demanding cyclic products of magnetic and biological significance will be discussed. Particular focus will be on the application of quaternization of threesubstituted amines and N-substituted azoles for production of organic salts and formation of magnetic ionic liquids by a template directed process. The feasibility of use of organic salts in the development of new pharmaceutical entities will be presented in the frame of such advantageous properties as low costs, simplicity in preparation and purification, controllable permeability through biological barriers. Previously, for organic salts more or less selective cytotoxicity against different types of cancer cells has been demonstrated. However, only antiproliferative activity has been presented with only few studies that have gone further to explore the mechanisms of the apparent cytotoxicity.