3 years ago

Phenoxypropanolamine derivatives as selective inhibitors of the 20S proteasome β1 and β 5 subunits

Phenoxypropanolamine derivatives as selective inhibitors of the 20S proteasome β1 and β 5 subunits
New series of thiophene-containing phenoxypropanolamines were synthesized and evaluated for their potency to inhibit the three proteolytic activities of the mammalian 20S proteasome. Noticeable inhibition of both ChT-L and PA activities was obtained with three compounds: one with unsubstituted phenoxypropanolamine group (7) and the two others with a p-Cl-substituted group (4 and 9). For three other compounds (3, 8 and 10), ChT-L activity alone was significantly inhibited. In silico docking performed on the β 5 and β 1 subunits bearing the respective ChT-L and PA catalytic sites showed features common to poses associated with active compounds. These features may constitute a selectivity criterion for structure-guided inhibitor design.

Publisher URL: www.sciencedirect.com/science

DOI: S0960894X17310557

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