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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

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

doi

10.1016/j.bmcl.2016.03.116

subject

Has Abstract

pub_date

2016-05-15 00:00:00

pages

2434-2437

issue

10

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(16)30347-X

journal_volume

26

pub_type

杂志文章

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