Substituted quinolines as noncovalent proteasome inhibitors.
Substituted quinolines as noncovalent proteasome inhibitors.
复制标题
取代喹啉作为非共价蛋白酶体抑制剂。
DOI：
10.1016/j.bmc.2016.04.005
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发表时间：
2016
影响因子：
3.5
通讯作者：
Tepe,JetzeJ
中科院分区：
文献类型：
--
作者：
McDaniel,TannerJ;Lansdell,TheresaA;Dissanayake,AmilaA;Azevedo,LaurenM;Claes,Jacob;Odom,AaronL;Tepe,JetzeJ
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 compound25inhibits the chymotryptic-like proteolytic activity of the proteasome (IC505.4 μM), representing a new class of nonpeptidic, noncovalent proteasome inhibitors.
