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

[Display omitted] •A novel squaramide-based scaffold for HDAC inhibition is proposed.•Inhibitors are optimized for topical route of administration.•Aqueous and organic solubility is optimized by crystal lattice perturbation.•Optimized HDAC inhibitors are class I, IIB and IV selective. A series of sq...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2018-09, Vol.28 (17), p.2985-2992
Hauptverfasser:	Fournier, Jean-François, Bhurruth-Alcor, Yushma, Musicki, Branislav, Aubert, Jérome, Aurelly, Michèle, Bouix-Peter, Claire, Bouquet, Karinne, Chantalat, Laurent, Delorme, Marion, Drean, Bénédicte, Duvert, Gwenaelle, Fleury-Bregeot, Nicolas, Gauthier, Blanche, Grisendi, Karine, Harris, Craig S., Hennequin, Laurent F., Isabet, Tatiana, Joly, Florence, Lafitte, Guillaume, Millois, Corinne, Morgentin, Rémy, Pascau, Jonathan, Piwnica, David, Rival, Yves, Soulet, Catherine, Thoreau, Étienne, Tomas, Loïc
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Apoptosis - drug effects Cell Line, Tumor Cell Proliferation - drug effects Crystallography, X-Ray CTCL Dose-Response Relationship, Drug Drug Screening Assays, Antitumor HDAC inhibitors Histone Deacetylase 1 - antagonists & inhibitors Histone Deacetylase 1 - metabolism Histone Deacetylase 2 - antagonists & inhibitors Histone Deacetylase 2 - metabolism Histone Deacetylase Inhibitors - chemical synthesis Histone Deacetylase Inhibitors - chemistry Histone Deacetylase Inhibitors - pharmacology Humans Lymphoma, T-Cell, Cutaneous - drug therapy Lymphoma, T-Cell, Cutaneous - metabolism Lymphoma, T-Cell, Cutaneous - pathology Models, Molecular Molecular Structure Mycosis fungoides Quinine - analogs & derivatives Quinine - chemical synthesis Quinine - chemistry Quinine - pharmacology Skin Neoplasms - drug therapy Skin Neoplasms - metabolism Skin Neoplasms - pathology Solubility Squaramide Structure-Activity Relationship Topical
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