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Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma |
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| Authors: | Jean-François Fournier Yushma Bhurruth-Alcor Branislav Musicki Jérome Aubert Michèle Aurelly Claire Bouix-Peter Karinne Bouquet Laurent Chantalat Marion Delorme Bénédicte Drean Gwenaelle Duvert Nicolas Fleury-Bregeot Blanche Gauthier Karine Grisendi Craig S. Harris Laurent F. Hennequin Tatiana Isabet Florence Joly Loïc Tomas |
| Affiliation: | 1. Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France;2. Edelris, 115 Avenue Lacassagne, 69003 Lyon, France;3. Synchrotron Soleil, L''Orme des Merisiers, Saint-Aubin – BP 48, 91192 Gif-sur-Yvette Cedex, France |
| Abstract: | 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. |
| Keywords: | XNBWKNWCSWBFRL-UHFFFAOYSA-N WOGPSXAJPRAXBA-UHFFFAOYSA-N RHUMXXCHLQENCI-UHFFFAOYSA-N HDAC inhibitors Squaramide CTCL Topical Corresponding author. |
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