This mini-review summarizes the development of the derivatives and conjugates of Amphotericin B (AMB) which have not been clinically applied so far but are therapeutically promising. Effects of chemical modifications of AMB upon biological activities of the resulting derivatives are discussed. The examples presented include variation of functional groups in AMB, covalent conjugates with other molecules, poly(ethylene glycols) and polysaccharides. Possibilities of targeted delivery of AMB are discussed.