Work

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

Year: 2017

Type: article

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.

Source: ChemMedChem

DOI: 10.1002/cmdc.201700630

Authors: Katherine M. Byrd, Caitlin N. Kent, Brian S. J. Blagg

Institution: University of Notre Dame

Language: English

Topic: Heat shock proteins research

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: green

Funders: National Institutes of Health, National Cancer Institute, National Institute of General Medical Sciences