Total Synthesis and Antitumor Activity of ZK‐EPO: The First Fully Synthetic Epothilone in Clinical Development
2006; Wiley; Volume: 118; Issue: 47 Linguagem: Inglês
10.1002/ange.200602785
ISSN1521-3757
AutoresUlrich Klar, Bernd Buchmann, Wolfgang Schwede, Werner Skuballa, Jens Hoffmann, Rosemarie B. Lichtner,
Tópico(s)Advanced Synthetic Organic Chemistry
ResumoAngewandte ChemieVolume 118, Issue 47 p. 8110-8116 Zuschrift Total Synthesis and Antitumor Activity of ZK-EPO: The First Fully Synthetic Epothilone in Clinical Development† Ulrich Klar Dr., Ulrich Klar Dr. [email protected] Schering AG, Research Center Europe, Müllerstrasse 178, 13342 Berlin, Germany, Fax: (+49) 30-468-92635 http://www.schering.deSearch for more papers by this authorBernd Buchmann Dr., Bernd Buchmann Dr. Schering AG, Research Center Europe, Müllerstrasse 178, 13342 Berlin, Germany, Fax: (+49) 30-468-92635 http://www.schering.deSearch for more papers by this authorWolfgang Schwede Dr., Wolfgang Schwede Dr. Schering AG, Research Center Europe, Müllerstrasse 178, 13342 Berlin, Germany, Fax: (+49) 30-468-92635 http://www.schering.deSearch for more papers by this authorWerner Skuballa Prof., Werner Skuballa Prof. Schering AG, Research Center Europe, Müllerstrasse 178, 13342 Berlin, Germany, Fax: (+49) 30-468-92635 http://www.schering.deSearch for more papers by this authorJens Hoffmann Dr., Jens Hoffmann Dr. Schering AG, Research Center Europe, Müllerstrasse 178, 13342 Berlin, Germany, Fax: (+49) 30-468-92635 http://www.schering.deSearch for more papers by this authorRosemarie B. Lichtner Dr., Rosemarie B. Lichtner Dr. Schering AG, Research Center Europe, Müllerstrasse 178, 13342 Berlin, Germany, Fax: (+49) 30-468-92635 http://www.schering.deSearch for more papers by this author Ulrich Klar Dr., Ulrich Klar Dr. [email protected] Schering AG, Research Center Europe, Müllerstrasse 178, 13342 Berlin, Germany, Fax: (+49) 30-468-92635 http://www.schering.deSearch for more papers by this authorBernd Buchmann Dr., Bernd Buchmann Dr. Schering AG, Research Center Europe, Müllerstrasse 178, 13342 Berlin, Germany, Fax: (+49) 30-468-92635 http://www.schering.deSearch for more papers by this authorWolfgang Schwede Dr., Wolfgang Schwede Dr. Schering AG, Research Center Europe, Müllerstrasse 178, 13342 Berlin, Germany, Fax: (+49) 30-468-92635 http://www.schering.deSearch for more papers by this authorWerner Skuballa Prof., Werner Skuballa Prof. Schering AG, Research Center Europe, Müllerstrasse 178, 13342 Berlin, Germany, Fax: (+49) 30-468-92635 http://www.schering.deSearch for more papers by this authorJens Hoffmann Dr., Jens Hoffmann Dr. Schering AG, Research Center Europe, Müllerstrasse 178, 13342 Berlin, Germany, Fax: (+49) 30-468-92635 http://www.schering.deSearch for more papers by this authorRosemarie B. Lichtner Dr., Rosemarie B. Lichtner Dr. Schering AG, Research Center Europe, Müllerstrasse 178, 13342 Berlin, Germany, Fax: (+49) 30-468-92635 http://www.schering.deSearch for more papers by this author First published: 27 November 2006 https://doi.org/10.1002/ange.200602785Citations: 14 † We thank Siegfried Bäsler, Stefan Barm, Angela Bieseke, Klaus Burmeister, Klaus Cornelius, Gisbert Depke, Ralf Günther, Wolfgang Halfbrodt, Frank Halwass, Karola Henschel, Hiltraud Hillmann, Klaus-Dieter Joachim, Frank Kuczynski, Hue-Quan Lao, Günter Michl, Gerhard Neumann, Christian Pingel, Ingrid Pissarczyk, Peter Pretsch, Bodo Röhr, Oliver Schenk, Michael Schirner, Jürgen Skupsch, Marion Slopianka, Daniela Wrobel, and Henk Zimmermann for their excellent scientific and technical assistance. Read the full textAboutPDF ToolsRequest permissionAdd to favorites ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Share a linkShare onEmailFacebookTwitterLinkedInRedditWechat Graphical Abstract Auf dem Prüfstand: Unter 350 aktiven Epothilon-Analoga, die hoch konvergent synthetisiert wurden, wurde das abgebildete ZK-EPO wegen seiner hervorragenden Daten in präklinischen Tests für die klinische Entwicklung ausgewählt. Die Verbindung ist aktiver und effizienter als Taxane (z. B. Paclitaxel) und Epothilone der zweiten Generation, sie wird gut in Zellen aufgenommen, nicht durch Effluxmechanismen erkannt und überzeugt durch ein besseres Therapiefenster. 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