Design, Synthesis, Radiosynthesis and Biological Evaluation of Fenretinide Analogues as Anticancer and Metabolic Syndrome-Preventive Agents.
Animals
Antineoplastic Agents
/ chemical synthesis
Cell Differentiation
/ drug effects
Cell Proliferation
/ drug effects
Cell Survival
/ drug effects
Cells, Cultured
Dose-Response Relationship, Drug
Drug Design
Drug Screening Assays, Antitumor
Fenretinide
/ chemical synthesis
Fluorine Radioisotopes
Humans
Lipids
/ antagonists & inhibitors
Metabolic Syndrome
/ prevention & control
Mice
Molecular Structure
Positron-Emission Tomography
Retinoids
/ analysis
Structure-Activity Relationship
cancer
drug discovery
fenretinide
metabolic syndrome
radiopharmaceuticals
Journal
ChemMedChem
ISSN: 1860-7187
Titre abrégé: ChemMedChem
Pays: Germany
ID NLM: 101259013
Informations de publication
Date de publication:
19 08 2020
19 08 2020
Historique:
received:
05
03
2020
revised:
21
05
2020
pubmed:
5
6
2020
medline:
16
6
2021
entrez:
5
6
2020
Statut:
ppublish
Résumé
Fenretinide (4-HPR) is a synthetic derivative of all-trans-retinoic acid (ATRA) characterised by improved therapeutic properties and toxicological profile relative to ATRA. 4-HPR has been mostly investigated as an anti-cancer agent, but recent studies showed its promising therapeutic potential for preventing metabolic syndrome. Several biological targets are involved in 4-HPR's activity, leading to the potential use of this molecule for treating different pathologies. However, although 4-HPR displays quite well-understood multitarget promiscuity with regards to pharmacology, interpreting its precise physiological role remains challenging. In addition, despite promising results in vitro, the clinical efficacy of 4-HPR as a chemotherapeutic agent has not been satisfactory so far. Herein, we describe the preparation of a library of 4-HPR analogues, followed by the biological evaluation of their anti-cancer and anti-obesity/diabetic properties. The click-type analogue 3 b showed good capacity to reduce the amount of lipid accumulation in 3T3-L1 adipocytes during differentiation. Furthermore, it showed an IC
Identifiants
pubmed: 32497314
doi: 10.1002/cmdc.202000143
doi:
Substances chimiques
Antineoplastic Agents
0
Fluorine Radioisotopes
0
Lipids
0
Retinoids
0
Fenretinide
187EJ7QEXL
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
1579-1590Subventions
Organisme : British Heart Foundation
ID : PG/16/90/32518
Pays : United Kingdom
Informations de copyright
© 2020 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.
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