1 research outputs found
Development of Noviomimetics as C‑Terminal Hsp90 Inhibitors
KU-32 and KU-596 are novobiocin-derived,
C-terminal heat shock
protein 90 (Hsp90) modulators that induce Hsp70 levels and manifest
neuroprotective activity. However, the synthetically complex noviose
sugar requires 10 steps to prepare, which makes translational development
difficult. In this study, we developed a series of “noviomimetic”
analogues of KU-596, which contain noviose surrogates that can be
easily prepared, while maintaining the ability to induce Hsp70 levels.
Both sugar and sugar analogues were designed, synthesized, and evaluated
in a luciferase reporter assay, which identified compound <b>37</b>, a benzyl containing noviomimetic, as the most potent inducer of
Hsp70