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Substituted quinolines as noncovalent proteasome inhibitors.

Abstract：

:Screening of a library of diverse heterocyclic scaffolds identified substituted quinolines as inhibitors of the human proteasome. The heterocyclic library was prepared via a novel titanium-catalyzed multicomponent coupling reaction, which rendered a diverse set of isoxazoles, pyrimidines, pyrroles, pyrazoles and quinolines. SAR of the parent lead compound indicated that hydrophobic residues on the benzo-moiety significantly improved potency. Lead compound 25 inhibits the chymotryptic-like proteolytic activity of the proteasome (IC50 5.4μM), representing a new class of nonpeptidic, noncovalent proteasome inhibitors.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

McDaniel TJ,Lansdell TA,Dissanayake AA,Azevedo LM,Claes J,Odom AL,Tepe JJ

doi

10.1016/j.bmc.2016.04.005

subject

Has Abstract

pub_date

2016-06-01 00:00:00

pages

2441-50

issue

11

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(16)30239-5

journal_volume

24

pub_type

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