Structure, Biological Activity and Synthesis of Polyamine Analogues and Conjugates

摘要

The structure and the biological significance of naturally occurring and synthetic polyamine analogues and conjugates are presented and the available methodologies for their synthesis are described. These methodologies involve either the selective functionalization of the amino functions, using suitable protecting groups or acylating agents, or fragment synthesis protocols. The latter employ suitable amino components and simple reactions, like Michael addition to α,β-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 solution as well as in the solid phase are discussed.