|
|||||
|
|
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 2 |
|
| Authors: | Colletti S L Myers R W Darkin-Rattray S J Gurnett A M Dulski P M Galuska S Allocco J J Ayer M B Li C Lim J Crumley T M Cannova C Schmatz D M Wyvratt M J Fisher M H Meinke P T |
| Affiliation: | Merck Research Laboratories, Merck & Co., Inc., Rahway, NJ 07065, USA. steve_colletti@merck.com |
| Abstract: | Recently isolated at Merck, apicidin inhibits both mammalian and protozoan histone deacetylases (HDACs). The conversion of apicidin, a nonselective nanomolar inhibitor of HDACs, into a series of picomolar indole-modified and parasite-selective tryptophan-replacement analogues is described within this structure-activity study. |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ | |