Discovery of N-Arylsulfonyl-Indole-2-Carboxamide Derivatives as Galectin-3 and Galectin-8 C-Terminal Domain Inhibitors.

ABSTRACT: Both galectin-3 and galectin-8 are involved in cell adhesion, migration, apoptosis, angiogenesis, and inflammatory processes by recognizing galactose-containing glycoproteins. Inhibiting galectin-3/8 activities is a potential treatment for cancer and tissue fibrosis. Herein, a series of novel N-arylsulfonyl-5-aryloxy-indole-2-carboxamide derivatives was disclosed as dual inhibitors toward galectin-3 and galectin-8 C-terminal domain with K_d values of low micromolar level (Cpd53, gal-3: K_d= 4.12 μM, gal-8C: K_d= 6.04 μM; Cpd57, gal-3: K_d= 12.8 μM, gal-8C: K_d= 2.06 μM), which are the most potent and selective noncarbohydrate-based inhibitors toward gal-3/8

SUBMITTER: Zhang H 

PROVIDER: S-EPMC10510525 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature