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Discovery of pyrimidyl-5-hydroxamic acids as new potent histone deacetylase inhibitors
Authors:Angibaud Patrick  Arts Janine  Van Emelen Kristof  Poncelet Virginie  Pilatte Isabelle  Roux Bruno  Van Brandt Sven  Verdonck Marc  De Winter Hans  Ten Holte Peter  Marien Ann  Floren Wim  Janssens Boudewijn  Van Dun Jacky  Aerts An  Van Gompel Jacky  Gaurrand Sandrine  Queguiner Laurence  Argoullon Jean-Michel  Van Hijfte Luc  Freyne Eddy  Janicot Michel
Institution:Johnson&Johnson Pharmaceutical Research&Development (J&JPRD), Medicinal Chemistry Department, campus de Maigremont BP615, 27106 Val de Reuil, France. pangibau@PRDFR.jnj.com
Abstract:A series of pyrimidyl-5-hydroxamic acids was prepared for evaluation as inhibitors of histone deacetylase (HDAC). Amino-2-pyrimidinyl can be used as a linker to provide HDAC inhibitors of good enzymatic potency.
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