Skip to main content
Journal cover image

Phosphorus-based SAHA analogues as histone deacetylase inhibitors.

Publication ,  Journal Article
Kapustin, GV; Fejér, G; Gronlund, JL; McCafferty, DG; Seto, E; Etzkorn, FA
Published in: Organic letters
August 2003

[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.

Duke Scholars

Published In

Organic letters

DOI

EISSN

1523-7052

ISSN

1523-7060

Publication Date

August 2003

Volume

5

Issue

17

Start / End Page

3053 / 3056

Related Subject Headings

  • Vorinostat
  • Tumor Cells, Cultured
  • Recombinant Proteins
  • Ovarian Neoplasms
  • Organophosphorus Compounds
  • Organic Chemistry
  • Inhibitory Concentration 50
  • Hydroxamic Acids
  • Humans
  • Histone Deacetylase Inhibitors
 

Citation

APA
Chicago
ICMJE
MLA
NLM
Kapustin, G. V., Fejér, G., Gronlund, J. L., McCafferty, D. G., Seto, E., & Etzkorn, F. A. (2003). Phosphorus-based SAHA analogues as histone deacetylase inhibitors. Organic Letters, 5(17), 3053–3056. https://doi.org/10.1021/ol035056n
Kapustin, Galina V., György Fejér, Jennifer L. Gronlund, Dewey G. McCafferty, Edward Seto, and Felicia A. Etzkorn. “Phosphorus-based SAHA analogues as histone deacetylase inhibitors.Organic Letters 5, no. 17 (August 2003): 3053–56. https://doi.org/10.1021/ol035056n.
Kapustin GV, Fejér G, Gronlund JL, McCafferty DG, Seto E, Etzkorn FA. Phosphorus-based SAHA analogues as histone deacetylase inhibitors. Organic letters. 2003 Aug;5(17):3053–6.
Kapustin, Galina V., et al. “Phosphorus-based SAHA analogues as histone deacetylase inhibitors.Organic Letters, vol. 5, no. 17, Aug. 2003, pp. 3053–56. Epmc, doi:10.1021/ol035056n.
Kapustin GV, Fejér G, Gronlund JL, McCafferty DG, Seto E, Etzkorn FA. Phosphorus-based SAHA analogues as histone deacetylase inhibitors. Organic letters. 2003 Aug;5(17):3053–3056.
Journal cover image

Published In

Organic letters

DOI

EISSN

1523-7052

ISSN

1523-7060

Publication Date

August 2003

Volume

5

Issue

17

Start / End Page

3053 / 3056

Related Subject Headings

  • Vorinostat
  • Tumor Cells, Cultured
  • Recombinant Proteins
  • Ovarian Neoplasms
  • Organophosphorus Compounds
  • Organic Chemistry
  • Inhibitory Concentration 50
  • Hydroxamic Acids
  • Humans
  • Histone Deacetylase Inhibitors