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Total Synthesis and Antitumor Activity of ZK‐EPO: The First Fully Synthetic Epothilone in Clinical Development
Author(s) -
Klar Ulrich,
Buchmann Bernd,
Schwede Wolfgang,
Skuballa Werner,
Hoffmann Jens,
Lichtner Rosemarie B.
Publication year - 2006
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200602785
Subject(s) - epothilones , epothilone , paclitaxel , therapeutic window , chemistry , pharmacology , efflux , computer science , stereochemistry , medicine , biochemistry , cancer
Going to trial : From about 350 active epothilone analogues synthesized by a highly convergent synthesis, one (ZK‐EPO, see picture) has been chosen for clinical development on the basis of its outstanding preclinical data. This compound exhibits higher activity and efficacy than taxanes (e.g. paclitaxel) and second‐generation epothilones, a fast and efficient cellular uptake, no recognition by efflux mechanisms, and an improved therapeutic window.