Synthesis and biological evaluation of amphotericin B derivatives

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Synthesis and biological evaluation of amphotericin B derivatives

Astrid A. Volmer,^a Alex M. Szpilman^a and Erick M. Carreira*^a

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* Corresponding authors

^a Laboratorium für Organische Chemie der ETH-Zürich, HCI H 335, Wolfgang Pauli Strasse 10, Zurich, Switzerland
E-mail: carreira@org.chem.ethz.ch
Fax: +41 44 632 1328
Tel: +41 44 632 2830

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.

Graphical abstract: Synthesis and biological evaluation of amphotericin B derivatives

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Article information

DOI: https://doi.org/10.1039/B820743G
Article type: Review Article
Submitted: 18 Dec 2009
First published: 16 Jun 2010

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Nat. Prod. Rep., 2010,27, 1329-1349

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