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Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma.
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.
Afiliación
  • Fournier JF; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France. Electronic address: jean-francois.fournier@umontreal.ca.
  • Bhurruth-Alcor Y; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Musicki B; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Aubert J; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Aurelly M; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Bouix-Peter C; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Bouquet K; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Chantalat L; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Delorme M; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Drean B; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Duvert G; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Fleury-Bregeot N; Edelris, 115 Avenue Lacassagne, 69003 Lyon, France.
  • Gauthier B; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Grisendi K; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Harris CS; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Hennequin LF; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Isabet T; Synchrotron Soleil, L'Orme des Merisiers, Saint-Aubin - BP 48, 91192 Gif-sur-Yvette Cedex, France.
  • Joly F; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Lafitte G; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Millois C; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Morgentin R; Edelris, 115 Avenue Lacassagne, 69003 Lyon, France.
  • Pascau J; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Piwnica D; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Rival Y; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Soulet C; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Thoreau É; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • Tomas L; Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
Bioorg Med Chem Lett ; 28(17): 2985-2992, 2018 09 15.
Article en En | MEDLINE | ID: mdl-30122227
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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Quinina / Neoplasias Cutáneas / Linfoma Cutáneo de Células T / Histona Desacetilasa 1 / Histona Desacetilasa 2 / Inhibidores de Histona Desacetilasas / Antineoplásicos Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2018 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Quinina / Neoplasias Cutáneas / Linfoma Cutáneo de Células T / Histona Desacetilasa 1 / Histona Desacetilasa 2 / Inhibidores de Histona Desacetilasas / Antineoplásicos Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2018 Tipo del documento: Article Pais de publicación: Reino Unido