3 years ago

Synthesis and biological evaluation of stilbene analogs as Hsp90 C-terminal inhibitors

katherine byrd, Brian Blagg, Caitlyn kent
The design, synthesis and biological evaluation of stilbene-based novobiocin analogs is reported. Replacement of the biaryl amide side chain with a triazole side chain produced compounds that exhibited good anti-proliferative activities. Hsp90 inhibition was observed when N-methyl piperidine was replaced with acyclic tertiary amines on the stilbene analogs that also contain a triazole-derived side chain. These studies revealed that ~24 Å is the optimal length for compounds that exhibit good anti-proliferative activity as a result of Hsp90 inhibition.

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1002/cmdc.201700630

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