Phosphorus-based SAHA analogues as histone deacetylase inhibitors.
Journal Article (Journal Article)
[structure: see text] Three analogues of suberoyl anilide hydroxamic acid (SAHA) with phosphorus metal-chelating functionalities were synthesized as inhibitors of histone deacetylases (HDACs). The compounds showed weak activity for HeLa nuclear extracts (IC(50) = 0.57-6.1 mM), HDAC8 (IC(50) = 0.28-0.41 mM), and histone-deacetylase-like protein (HDLP, IC(50) = 0.33-1.9 mM), suggesting that the transition state of HDAC is not analogous to zinc proteases. Antiproliferative activity against A2780 cancer cells (IC(50) = 0.11-0.12 mM), comparable to SAHA (0.15 mM), was observed.
Full Text
Duke Authors
Cited Authors
- Kapustin, GV; Fejér, G; Gronlund, JL; McCafferty, DG; Seto, E; Etzkorn, FA
Published Date
- August 2003
Published In
Volume / Issue
- 5 / 17
Start / End Page
- 3053 - 3056
PubMed ID
- 12916979
Electronic International Standard Serial Number (EISSN)
- 1523-7052
International Standard Serial Number (ISSN)
- 1523-7060
Digital Object Identifier (DOI)
- 10.1021/ol035056n
Language
- eng