Silatranes compounds, R-Si(OCH2CH2)3N, possess astounding physical-chemical properties (high dipole moment, easy polarizability of the R-Si bond, reliability to hy-drolysis) and valuable biological activity. This kind of activity is definitely due to the easier (because of hydrogen bonds formation and dipole-dipole coupling) adsorption of silatranes on the surface of cell membranes and active transport of their molecules into the cells, which is really important to drug discovery and design. The variety of silatranes applications has attracted the interest in the modification of their exocyclic functional substituents (amino- and thioalkylsilatranes are known as precursors for the synthesis of new compounds exhibiting interesting and valuable properties). On the other hand, the 5-bromosalicylaldehyde containing Schiff bases have antitumor activity and are applied for manufacturing of anti-cancer drugs. These Schiff bases has unique biological activity and can be used as low toxic in design and synthesis, and has got several applications like antibacterial and fungal, anti-inflammatory, anti-tubercular, anti-oxidant, and kills para-sitic worms. Molecular hybridization is a method of combining two or more pharmaco-phoric units into one molecule being preferred in design of new compounds. This was successfully used to access, in particular, new silatrane hybrids with biomedical and other activities.