Total Synthesis and Antitumor Activity of ZK-EPO: The First Fully Synthetic Epothilone in Clinical Development

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. paclita...

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Bibliographic Details
Published in:Angewandte Chemie International Edition 2006-12, Vol.45 (47), p.7942-7948
Main Authors: Klar, Ulrich, Buchmann, Bernd, Schwede, Wolfgang, Skuballa, Werner, Hoffmann, Jens, Lichtner, Rosemarie B.
Format: Article
Language:English
Subjects:
4-Butyrolactone - analogs & derivatives
4-Butyrolactone - chemistry
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
clinical development
Cyclization
epothilones
Epothilones - chemical synthesis
Epothilones - pharmacology
HeLa Cells
Humans
Inhibitory Concentration 50
Models, Chemical
natural products
Time Factors
total synthesis
Tumor Cells, Cultured - drug effects
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Summary: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.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.200602785