Cover Picture: Total Synthesis and Antitumor Activity of ZK-EPO: The First Fully Synthetic Epothilone in Clinical Development (Angew. Chem. Int. Ed. 47/2006)

✍ Scribed by Ulrich Klar; Bernd Buchmann; Wolfgang Schwede; Werner Skuballa; Jens Hoffmann; Rosemarie B. Lichtner

• Publisher: John Wiley and Sons
• Year: 2006
• Tongue: English
• Weight: 161 KB
• Volume: 45
• Category: Article
• ISSN: 0044-8249
• DOI: 10.1002/anie.200690162

✦ Synopsis

Nature is a brilliant architect for the design of compounds with interesting biological functions. Epothilone B (top), a metabolite of myxobacteria (fruiting body in background), served as the lead structure for the development of an anticancer drug candidate. Optimization efforts led to ZK‐EPO (bottom) as a candidate for clinical development. ZK‐EPO has an improved therapeutic window and is not recognized by multidrug‐resistance efflux pumps. Its total synthesis starting from simple compounds (blue) is described by U. Klar et al. on page 7942 ff.