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

Abstract：

: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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Marastoni E,Bartoli S,Berettoni M,Cipollone A,Ettorre A,Fincham CI,Mauro S,Paris M,Porcelloni M,Bigioni M,Binaschi M,Nardelli F,Parlani M,Maggi CA,Fattori D

doi

10.1016/j.bmcl.2013.05.053

subject

Has Abstract

pub_date

2013-07-15 00:00:00

pages

4091-5

issue

14

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)00648-3

journal_volume

23

pub_type

杂志文章

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