Broad spectrum antiprotozoal agents that inhibit histone deacetylase: Structure-activity relationships of apicidin. Part 1

Authors
Colletti, SL Myers, RW Darkin-Rattray, SJ Gurnett, AM Dulski, PM Galuska, S Allocco, JJ Ayer, MB Li, CS Lim, J Crumley, TM Cannova, C Schmatz, DM Wyvratt, MJ Fisher, MH Meinke, PT
Citation
Sl. Colletti et al., Broad spectrum antiprotozoal agents that inhibit histone deacetylase: Structure-activity relationships of apicidin. Part 1, BIOORG MED, 11(2), 2001, pp. 107-111
Citations number
26
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
2
Year of publication
2001
Pages
107 - 111
Database
ISI
SICI code
0960-894X(20010122)11:2<107:BSAATI>2.0.ZU;2-2
Abstract
Apicidin, a natural product recently isolated at Merck, inhibits both mamma lian and protozoan histone deacetylases (HDACs). The conversion of apicidin , a nanomolar inhibitor of HDACs, into a series of side-chain analogues tha t display picomolar enzyme affinity is described within this structure-acti vity study. (C) 2001 Elsevier Science Ltd. All rights reserved.