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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 - Reports
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/1521-3773(20020118)41:2<195::aid-anie195>3.0.co;2-i
Subject(s) - cytotoxicity , front cover , chemistry , polymer , microtiter plate , combinatorial chemistry , nanotechnology , cover (algebra) , materials science , chromatography , biochemistry , organic chemistry , in vitro , mechanical engineering , engineering
The cover picture shows schematically the 11‐step synthesis of 6‐ epi ‐dysidiolide on a solid support. By means of this extraordinarily demanding and long solid‐phase synthesis a small library of analogues of the Cdc25 protein phosphatase inhibitor dysidiolide was synthesized. This synthesis demonstrates that the solid‐phase synthesis of natural products and compound libraries derived from them is feasible. This is a decisive cornerstone of a new principle for enhancing the efficiency of the hit‐ and lead‐finding processes in pharmaceutical research based on natural products and their interaction with protein domains. Electron microscopy pictures of polymer beads and tumor cells are shown in the background. A 2‐nm‐thick gold layer was vaporized on to the resin beads. Tumor cells floating in front of the beads were employed in a cytotoxicity assay. The results of the assay are readily seen on the microtiter plates with the naked eye: living cells reduce a yellow tetrazolium salt to a red‐violet dye. A detailed description of the study is reported by H. Waldmann et al. on p. 307 ff.