Characterization of a Novel Family of Contilisant + Belinostat Multitarget Small Molecules in Glioblastoma.

ABSTRACT: Background: Glioblastoma is the most common and malignant primary brain tumor in adults, with current treatment presenting limited effectiveness. Therapeutic resistance stems largely from its marked molecular and cellular heterogeneity. Multitarget small molecules (MSMs) have emerged as a promising strategy for treating complex diseases such as cancer. In the present work, we generated a novel family of indole-based MSMs engineered to inhibit histone deacetylases (HDACs), monoamine oxidases (MAOs) and cholinesterases (ChEs) while simultaneously acting as histamine H₃ receptor (H3R) antagonists and sigma-1 receptor (S1R) agonists. Methods: To accomplish this, we combined selected pharmacophoric moieties from the parent compounds Contilisant and the HDAC pan-inhibito

SUBMITTER: Artetxe-Zurutuza A 

PROVIDER: S-EPMC12845422 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature