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Identification of new γ-hydroxybutenolides that preferentially inhibit the activity of mPGES-1.

Abstract：

:Microsomal prostaglandin E(2) synthase-1 (mPGES-1) has been recognized as novel, promising drug target for anti-inflammatory and anticancer drugs. mPGES-1 catalyzes the synthesis of the inducible prostaglandin E(2) in response to pro-inflammatory stimuli, rendering this enzyme extremely interesting in drug discovery process owing to the drastic reduction of the severe side effects typical for traditional non-steroidal anti-inflammatory drugs. In the course of our investigations focused on this topic, we identified two interesting molecules bearing the γ-hydroxybutenolide scaffold which potently inhibit the activity of mPGES-1. Notably, the lead compound 2c that inhibited mPGES-1 with IC(50) = 0.9 μM, did not affect other related enzymes within the arachidonic acid cascade.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

De Simone R,Bruno I,Riccio R,Stadler K,Bauer J,Schaible AM,Laufer S,Werz O

doi

10.1016/j.bmc.2012.06.032

subject

Has Abstract

pub_date

2012-08-15 00:00:00

pages

5012-6

issue

16

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(12)00510-X

journal_volume

20

pub_type

杂志文章

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