Contilisant+Belinostat hybrids, as new multi-target-directed polyfunctionalized indole derivatives able to inhibit histone deacetylase/cholinesterase/monoamine oxidase enzymes, and modulate histamine 3/sigma 1/5-HT6/dopamine 3 receptors for the treatment of cancer and neurodegenerative diseases

Herein we describe the design and synthesis of Contilisant+Belinostat hybrids as polyfunctionalized indole derivatives for the treatment of a broad diversity of cancers and neurodegenerative diseases, such as glioblastoma, and Alzheimer’s disease (AD). The new Contilisant+Belinostat hybrids have been designed as a Multi-Target-Directed (MTD) small molecules, able to inhibit HDAC6, cholinesterase and monoamine oxidase enzymes, and modulate histamine 3, sigma 1, 5-HT6, and dopamine 3 receptors. Contilisant+Belionostat hybrids has been submitted to biological evaluation in suitable in vitro and vivo glioblastoma and AD models.