4.5 Article

Benzofused hydroxamic acids: Useful fragments for the preparation of histone deacetylase inhibitors. Part 1: Hit identification

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

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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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