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Cover Picture: Total Synthesis and Antitumor Activity of ZK‐EPO: The First Fully Synthetic Epothilone in Clinical Development (Angew. Chem. Int. Ed. 47/2006)
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 - Reports
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200690162
Subject(s) - epothilone , total synthesis , myxobacteria , metabolite , efflux , drug candidate , combinatorial chemistry , stereochemistry , chemistry , int , multiple drug resistance , therapeutic window , computational biology , pharmacology , drug , biology , biochemistry , antibiotics , computer science , genetics , bacteria , operating system
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.