期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 14, 页码 4091-4095出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.05.053
关键词
HDAC; Hydroxamic acids; Fragment approach
In the search for a new class of histone deacetylase inhibitors, we prepared a series of simple benzofused hydroxamic acids to find an anchoring fragment of minimal molecular weight. These initial hits, all belonging to the benzothiophene class, showed very good ligand efficiencies. Following these findings, a classical fragment growing approach was performed to increase binding affinity and cytotoxicity. (C) 2013 Elsevier Ltd. All rights reserved.
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