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
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.