1.
Bioorg Med Chem Lett
; 26(10): 2434-2437, 2016 05 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-27055940
RESUMEN
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.