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Synthesis and Biological Evaluation of Stilbene Analogues as Hsp90 C-Terminal Inhibitors.

ABSTRACT: The design, synthesis, and biological evaluation of stilbene-based novobiocin analogues is reported. Replacement of the biaryl amide side chain with a triazole side chain produced compounds that exhibited good antiproliferative activities. Heat shock protein 90 (Hsp90) inhibition was observed when N-methylpiperidine was replaced with acyclic tertiary amines on the stilbene analogues that also contain a triazole-derived side chain. These studies revealed that ?24?Å is the optimal length for compounds that exhibit good antiproliferative activity as a result of Hsp90 inhibition.

SUBMITTER: Byrd KM

PROVIDER: S-EPMC5892432 | biostudies-literature | 2017 Dec

REPOSITORIES: biostudies-literature

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Synthesis and Biological Evaluation of Stilbene Analogues as Hsp90 C-Terminal Inhibitors.

Byrd Katherine M KM Kent Caitlin N CN Blagg Brian S J BSJ

ChemMedChem 20171130 24

The design, synthesis, and biological evaluation of stilbene-based novobiocin analogues is reported. Replacement of the biaryl amide side chain with a triazole side chain produced compounds that exhibited good antiproliferative activities. Heat shock protein 90 (Hsp90) inhibition was observed when N-methylpiperidine was replaced with acyclic tertiary amines on the stilbene analogues that also contain a triazole-derived side chain. These studies revealed that ≈24 Å is the optimal length for compo ...[more]

PMID: 29058824

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