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ID: ALA3792380

Journal: Bioorg Med Chem Lett

Title: A sub-milligram-synthesis protocol for in vitro screening of HDAC11 inhibitors.

Authors: Tian Y, Jin J, Wang C, Lv W, Li X, Che X, Gong Y, Li Y, Li Q, Hou J, Wang PG, Shen J.

Abstract: This work demonstrated the high efficiency of a sub-milligram-synthesis based medicinal chemistry method. Totally 72 compounds, consisting a tri-substituted pyrrolidine core, were prepared. Around 0.1mg of each compound was solid-phase synthesized. Based on the additive property of UV absorptions of unconjugated chromophores of a molecule, these compounds were quantified by UV measurement. A hit, whose IC50 value was 1.2μM in HDAC11 inhibition assays, highlights the applicability of the approach reported here in future optimization works.

CiteXplore: 27055940

DOI: 10.1016/j.bmcl.2016.03.116