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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
Author(s) -
Brohm Dirk,
Metzger Susanne,
Bhargava Ajay,
Müller Oliver,
Lieb Folker,
Waldmann Herbert
Publication year - 2002
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/1521-3773(20020118)41:2<307::aid-anie307>3.0.co;2-1
Subject(s) - solid phase synthesis , chemical space , natural compound , chemistry , stereochemistry , nanotechnology , combinatorial chemistry , computer science , materials science , engineering , drug discovery , biochemical engineering , biochemistry , peptide
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.