This review summarizes the author's research in the field of bio-medical application of modified calixarenes as well as their nano-associates. The paper includes results of design and investigation of the calixarenes as intracellular transport modulators of Ca and Na cations, as well as effective and selective phosphatases inhibitors. The antibacterial and anticoagulant properties of series water-soluble positively or negatively charged calixarenes are described. Also, utilization of calixarenes for hierarchical formation of nanoparticles for nanobiotechnological application (DNA transfection and bio-imaging) is discussed.