Broad spectrum antiprotozoal agents that inhibit histone deacetylase: Structure-activity relationships of apicidin. Part 2

Citation
Sl. Colletti et al., Broad spectrum antiprotozoal agents that inhibit histone deacetylase: Structure-activity relationships of apicidin. Part 2, BIOORG MED, 11(2), 2001, pp. 113-117
Citations number
6
Language
INGLESE
art.tipo
Article
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960-894X → ACNP
Volume
11
Issue
2
Year of publication
2001
Pages
113 - 117
Database
ISI
SICI code
0960-894X(20010122)11:2<113:BSAATI>2.0.ZU;2-3
Abstract
Recently isolated at Merck, apicidin inhibits both mammalian and protozoan histone deacetylases (HDACs). The conversion of apicidin, a nonselective na nomolar inhibitor of HDACs, into a series of picomolar indole-modified and parasite-selective tryptophan-replacement analogues is described within thi s structure-activity study. (C) 2001 Elsevier Science Ltd. All rights reser ved.