Contilisant+Tubastatin A 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

01 September 2023, Version 1

Abstract

Herein we describe the design and synthesis of Contilisant+Tubastatin A hybrids as polyfunctionalized indole derivatives for the treatment of a broad diversity of cancers, such as glioblastoma. The new Contilisant+Tubastatin A 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+Tubastatin A hybrids have been submitted to biological evaluation in suitable in vitro and vivo glioblastoma models.

Supplementary materials

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Title
ubastatin A hybrids, as new multi-targetdirected polyfunctionalized indole derivatives
Description
Spectroscopic and analyitical data for all the final target compounds, and intermediates to prepare them
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