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- W1979193128 abstract "Recently, we developed a concept known as biology-oriented synthesis (BIOS), which targets the design and synthesis of small- to medium-sized compound libraries on the basis of genuine natural product templates to provide screening compounds with high biological relevance. We herein describe the parallel solution phase synthesis of two BIOS-based libraries starting from α-santonin (1). Modification of the sesquiterpene lactone 1 by introduction of a thiazole moiety followed by a Lewis-acid-mediated lactone opening yielded a first library of natural product analogues. An acid-mediated dienone–phenol rearrangement of 1 and a subsequent etherification/amidation sequence led to a second natural product-based library. After application of a fingerprint-based virtual screening on these compounds, the biological screening of 23 selected library members against 5-lipoxygenase resulted in the discovery of four potent novel inhibitors of this enzyme." @default.
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- W1979193128 date "2007-09-13" @default.
- W1979193128 modified "2023-10-07" @default.
- W1979193128 title "Natural Products in Parallel Chemistry––Novel 5-Lipoxygenase Inhibitors from BIOS-Based Libraries Starting from α-Santonin" @default.
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- W1979193128 doi "https://doi.org/10.1021/cc700098t" @default.
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