Synthesis and biological evaluation of amphotericin B derivatives

Abstract

Covering: 1955 to 2009

The preparation and biological properties of various AmB analogs and conjugates that have been studied since the introduction of AmB into the clinic over 50 years ago are reviewed. Amphotericin B (AmB) analogs prepared by semi-synthetic modifications as well as those produced via genetic modification of the AmB polyketide synthase cluster are discussed, thereby highlighting the complementary approaches. In addition, the review includes the synthesis of AmB conjugated to biomolecules such as sterols and reactive markers such as fluorescent dyes, as well as their application to further understand the mechanism of action of the parent compound.