Kobzar O. Potential inhibitors of protein tyrosine phosphatases based on tetraazamacrocycles and fullerenes

Synthetic derivatives of tetraazamacrocycles and fullerenes as protein tyrosine phosphatase inhibitors. Search and determination of behaviours and mechanisms of action of potential protein tyrosine phosphatase inhibitors based on the tetraazamacrocycles and fullerenes. Enzyme kinetics, spectral analysis methods, molecular docking, theoretical calculations. The ideas that explain the new possible mechanisms of physiological activity of tetraazamacrocycles and fullerene derivatives were proposed and developed. The possibilities of using the derivatives of tetraazamacrocycles and fullerenes as molecular platforms for designing the protein tyrosine phosphatase inhibitors were demonstrated. It was found that tetrakis-substituted cyclam and its analogs (cyclen and homocyclam) which contained four benzyl-a,a-difluoro-b-ketophosphonate groups were strong and selective inhibitors of T-cell protein tyrosine phosphatase. Together with this, fullerenes that were functionalized by carboxyl groups showed good effects and selectivity as inhibitors of protein tyrosine phosphatase CD45. The results can be useful in the field of bioorganic chemistry.