Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma

Autor: Catherine Soulet, Laurent F. Hennequin, Nicolas Fleury-Brégeot, Craig S. Harris, Blanche Gauthier, Gwenaëlle Duvert, Etienne Thoreau, Laurent Chantalat, Karine Grisendi, Jean-François Fournier, Jerome Aubert, Michèle Aurelly, Rémy Morgentin, Claire Bouix-Peter, Bénédicte Drean, Guillaume Lafitte, Yushma Bhurruth-Alcor, Florence Joly, Jonathan Pascau, Branislav Musicki, Yves Rival, David Piwnica, Karinne Bouquet, Marion Delorme, T. Isabet, Corinne Millois, Loïc Tomas
Rok vydání: 2018
Předmět:
Models
Molecular
0301 basic medicine
Skin Neoplasms
Clinical Biochemistry
Histone Deacetylase 2
Pharmaceutical Science
Antineoplastic Agents
Apoptosis
Histone Deacetylase 1
Pharmacology
Crystallography
X-Ray
Biochemistry
Structure-Activity Relationship
03 medical and health sciences
0302 clinical medicine
Cell Line
Tumor
Drug Discovery
Hydrolase
medicine
Humans
Solubility
Molecular Biology
Cell Proliferation
chemistry.chemical_classification
Mycosis fungoides
Dose-Response Relationship
Drug
Molecular Structure
Quinine
Organic Chemistry
Cutaneous T-cell lymphoma
Squaramide
medicine.disease
Lymphoma
T-Cell
Cutaneous
Histone Deacetylase Inhibitors
030104 developmental biology
Enzyme
chemistry
Cell culture
030220 oncology & carcinogenesis
Molecular Medicine
Histone deacetylase
Drug Screening Assays
Antitumor
Zdroj: Bioorganic & Medicinal Chemistry Letters. 28:2985-2992
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2018.06.029
Popis: A series of squaramide-based hydroxamic acids were designed, synthesized and evaluated against human HDAC enzyme. Squaramides were found to be potent in the Hut78 cell line, but initially suffered from low solubility. Leads with improved solubility and metabolic profiles were shown to be class I, IIB and IV selective.
Databáze: OpenAIRE
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