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Natural Products Are Biologically Validated Starting Points in Structural Space for Compound Library Development: Solid-Phase Synthesis of Dysidiolide-Derived Phosphatase Inhibitors This research was supported by the Fonds der Chemischen Industrie and the Bayer AG.

2002; Wiley; Volume: 41; Issue: 2 Linguagem: Inglês

10.1002/1521-3773(20020118)41

1521-3773

Dirk Brohm, Susanne Metzger, Ajay Bhargava, Oliver Müller, Folker Lieb, Herbert Waldmann,

Carbohydrate Chemistry and Synthesis

Angewandte Chemie International EditionVolume 41, Issue 2 p. 307-311 Communication Natural Products Are Biologically Validated Starting Points in Structural Space for Compound Library Development: Solid-Phase Synthesis of Dysidiolide-Derived Phosphatase Inhibitors Dirk Brohm Dipl.-Chem., Dirk Brohm Dipl.-Chem. Max-Planck-Institut für Molekulare Physiologie Abteilung Chemische Biologie Otto-Hahn-Straße 11, 44227 Dortmund, Germany, Fax: (+49) 231-133-2499 and Universität Dortmund, Fb. 3, Organische ChemieSearch for more papers by this authorSusanne Metzger Dr., Susanne Metzger Dr. Bayer AG, Pharma Forschung PH-R LSC-NP, Geb. 6200, 40789 Monheim, GermanySearch for more papers by this authorAjay Bhargava Dr., Ajay Bhargava Dr. Bayer Corporation 400 Morgan Lane, West Haven, CT 06525, USASearch for more papers by this authorOliver Müller Dr., Oliver Müller Dr. Max-Planck-Institut für Molekulare Physiologie Dortmund Abteilung Strukturelle Biologie Otto-Hahn-Strasse 11, 44227 Dortmund, GermanySearch for more papers by this authorFolker Lieb Dr., Folker Lieb Dr. Bayer AG, Zentrale Forschung und Entwicklung ZF-LSC-SH, Geb. Q 18, 51368 Leverkusen, GermanySearch for more papers by this authorHerbert Waldmann Prof. Dr., Herbert Waldmann Prof. Dr. [email protected] Max-Planck-Institut für Molekulare Physiologie Abteilung Chemische Biologie Otto-Hahn-Straße 11, 44227 Dortmund, Germany, Fax: (+49) 231-133-2499 and Universität Dortmund, Fb. 3, Organische ChemieSearch for more papers by this author Dirk Brohm Dipl.-Chem., Dirk Brohm Dipl.-Chem. Max-Planck-Institut für Molekulare Physiologie Abteilung Chemische Biologie Otto-Hahn-Straße 11, 44227 Dortmund, Germany, Fax: (+49) 231-133-2499 and Universität Dortmund, Fb. 3, Organische ChemieSearch for more papers by this authorSusanne Metzger Dr., Susanne Metzger Dr. Bayer AG, Pharma Forschung PH-R LSC-NP, Geb. 6200, 40789 Monheim, GermanySearch for more papers by this authorAjay Bhargava Dr., Ajay Bhargava Dr. Bayer Corporation 400 Morgan Lane, West Haven, CT 06525, USASearch for more papers by this authorOliver Müller Dr., Oliver Müller Dr. Max-Planck-Institut für Molekulare Physiologie Dortmund Abteilung Strukturelle Biologie Otto-Hahn-Strasse 11, 44227 Dortmund, GermanySearch for more papers by this authorFolker Lieb Dr., Folker Lieb Dr. Bayer AG, Zentrale Forschung und Entwicklung ZF-LSC-SH, Geb. Q 18, 51368 Leverkusen, GermanySearch for more papers by this authorHerbert Waldmann Prof. Dr., Herbert Waldmann Prof. Dr. [email protected] Max-Planck-Institut für Molekulare Physiologie Abteilung Chemische Biologie Otto-Hahn-Straße 11, 44227 Dortmund, Germany, Fax: (+49) 231-133-2499 and Universität Dortmund, Fb. 3, Organische ChemieSearch for more papers by this author First published: 18 January 2002 https://doi.org/10.1002/1521-3773(20020118)41:2 3.0.CO;2-1Citations: 128 This research was supported by the Fonds der Chemischen Industrie and the Bayer AG. Read the full textAboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation 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 A multistep solid-phase synthesis was used successfully to prepare a series of analogues (see picture) of the protein phosphatase inhibitor dysidiolide. The natural product and its analogues were prepared on a solid support over 8–12 linear steps with overall yields of 6–27 %. The analogues display pronounced antitumor activity in cell-based assays. References 1 Yu. I. Wolf, N. V. Grishin, E. V. Koonin, J. Mol. 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