Developing green and sustainable methods of organic synthesis, primarily for the synthesis of Biginelli, as well as quinoxalinone, benzoxazinone and benzylidene derivatives is subject of interest. All derivatives were exposed to pharmacological and biological studies. Generally, the most active compounds against specific tumors were differentiated. These molecules are currently in the next phase of preclinical trials. The second part of the achieved results is related to the synthesis and application of pharmacologically active ionic liquids. In forthcoming projects main goal will be to synthesized library of the tetrahydropyirimidnes as inhibitors of the specific biological targets.