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Design, synthesis and biological activity of 3-oxoamino-benzenesulfonamides as selective and reversible LSD1 inhibitors.

Abstract：

:Lysine specific demethylase 1 (LSD1) is a flavin-dependent amine oxidase that selectively removes one or two methyl groups from H3 at Lys4 and is recognized as a promising therapeutic target for cancer and other diseases. Here, a series of 3-oxoamino-benzenesulfonamides were synthesized and evaluated for their inhibitory activity against LSD1. Compounds 7b and 7h showed the most potent inhibition with the IC50 values of 9.5 and 6.9μM, respectively. Furthermore, the LSD1 inhibition of 7b and 7h were reversible and selective. Docking study presented the possible binding mode between 7b, 7h and the LSD1 active site. Taken together, 3-oxoamino-benzenesulfonamides may represent a new class of reversible LSD1 inhibitors and 7b and 7h were two hit compounds deserved further structural optimization.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Xi J,Xu S,Wu L,Ma T,Liu R,Liu YC,Deng D,Gu Y,Zhou J,Lan F,Zha X

doi

10.1016/j.bioorg.2017.04.006

subject

Has Abstract

pub_date

2017-06-01 00:00:00

pages

182-189

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(17)30036-6

journal_volume

72

pub_type

杂志文章

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