| Title : Contilistat, a new polyfunctionalized histone deacetylase inhibitor, showing potential capacity to inhibit cholinesterase\/monoamine oxidase enzymes, and modulate histamine 3, sigma 1, 5-HT6 and dopamine 3 receptors for the treatment of cancer and neurodegenerative diseases - Diez-Iriepa_2023_Chemrxiv__ |
| Author(s) : Diez-Iriepa D , Toledano-Pinedo M , Porro A , Almendros P , Rodriguez-Fernandez, MM , Samadi A , Iriepa I , Lopez-Munoz F , Artetxe-Zurutuza A , Matheu A , Marco-Contelles J |
| Ref : Chemrxiv , : , 2023 |
|
Abstract :
The present work describes the design, and synthesis of the polyfunctionalized indole derivative Contilistat for the treatment of a broad diversity of cancers, and neurodegenerative diseases such as glioblastoma, and Alzheimers disease (AD). Contilistat has been designed as a Multi-Target-Directed (MTD) small molecule, able to inhibit HDAC6, cholinesterase and monoamine oxidase enzymes, and modulate histamine 3, sigma 1, 5-HT6, and dopamine 3 receptors. Contilistat has been submitted to biological evaluation in suitable in vitro and vivo glioblastoma and AD models. |
| PubMedSearch : Diez-Iriepa_2023_Chemrxiv__ |
| PubMedID: |
| Inhibitor | Contilistat |
Diez-Iriepa D, Toledano-Pinedo M, Porro A, Almendros P, Rodriguez-Fernandez, MM, Samadi A, Iriepa I, Lopez-Munoz F, Artetxe-Zurutuza A, Matheu A, Marco-Contelles J (2023)
Contilistat, a new polyfunctionalized histone deacetylase inhibitor, showing potential capacity to inhibit cholinesterase\/monoamine oxidase enzymes, and modulate histamine 3, sigma 1, 5-HT6 and dopamine 3 receptors for the treatment of cancer and neurodegenerative diseases
Chemrxiv
:
Diez-Iriepa D, Toledano-Pinedo M, Porro A, Almendros P, Rodriguez-Fernandez, MM, Samadi A, Iriepa I, Lopez-Munoz F, Artetxe-Zurutuza A, Matheu A, Marco-Contelles J (2023)
Chemrxiv
: