Structure, biological activity and synthesis of polyamine analogues and conjugates

The structure and the biological significance of naturally occurring and sy nthetic polyamine analogues and conjugates are presented and the available methodologies for their synthesis are described. These methodologies involv e either the selective functionalization of the amino functions, using suit able protecting groups or acylating agents, or fragment synthesis protocols . The latter employ suitable amino components and simple reactions, like Mi chael addition to alpha,beta-unsaturated nitriles, alkylation of amines and sulfonamides, reductive alkylation and acylation followed by reduction of the thus-obtained amides, as key-reactions, or azides as key-intermediates, for the assembly of the polyamine skeleton. Syntheses performed in solutio n as well as in the solid phase are discussed.