New Derivatives of 2-(Cyclohexylamino)thiazol-4(5<i>H</i>)-one as Strong Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1: Synthesis, Antiproliferative and Redox-Modulating Activity.

ABSTRACT: In the present study, we synthesized nine new derivatives of 2-(cyclohexylamino)thiazol-4(5H)-one and evaluated their inhibitory activity against 11β-hydroxysteroid dehydrogenase type 1 and 2 (11β-HSD1 and 11β-HSD2), an enzyme responsible for the progression of metabolic disorders and cancers. All obtained derivatives showed inhibitory potential against 11β-HSD1, and four of them highly inhibited 11β-HSD1 activity with IC₅₀ values in the low micromolar range. The most active compound, 3h with IC₅₀ = 0.04 µM, became a more potent and selective inhibitor than carbenoxolone. In addition to inhibition of 11β-HSD1, we investigated the antitumor potential and effects on intracellular redox homeostasis of all newly synthesized compounds on five cancer cell line

SUBMITTER: Baumgart S 

PROVIDER: S-EPMC12470129 | biostudies-literature | 2025 Sep

REPOSITORIES: biostudies-literature