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Synthesis and cancer antiproliferative activity of new histone deacetylase inhibitors: hydrophilic hydroxamates and 2-aminobenzamide-containing derivatives.

Abstract
New series histone deacetylase inhibitors comprising a hydroxamic acid or 2-aminobenzamide group as a zinc-chelating function were synthesized and evaluated for antiproliferative activities against a panel of human cancer cells. The 2-aminobenzamide series inhibitors generally had the potency in cell growth inhibitions comparable to that of MS-275. Among them, the compound having a (3,4-difluorobenzyl)(2-hydroxyethyl)amino group at one end and a 2-aminobenzamide group at the other of molecule showed the most promising profile as an anticancer drug candidate, since it had a comparatively low toxicity as did MS-275 against a normal fibroblast cell CCD-1059SK. Additionally, the derivative exhibited a high recovery in human plasma stability test.
AuthorsY Nagaoka, T Maeda, Y Kawai, D Nakashima, T Oikawa, K Shimoke, T Ikeuchi, H Kuwajima, S Uesato
JournalEuropean journal of medicinal chemistry (Eur J Med Chem) Vol. 41 Issue 6 Pg. 697-708 (Jun 2006) ISSN: 0223-5234 [Print] France
PMID16584813 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Histone Deacetylase Inhibitors
  • Hydroxamic Acids
  • ortho-Aminobenzoates
  • anthranilamide
Topics
  • Antineoplastic Agents (blood, chemical synthesis, pharmacology)
  • Enzyme Inhibitors (blood, chemical synthesis, pharmacology)
  • Histone Deacetylase Inhibitors
  • Humans
  • Hydroxamic Acids (blood, chemical synthesis, pharmacology)
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry (methods)
  • Spectrophotometry, Infrared
  • ortho-Aminobenzoates (blood, chemical synthesis, pharmacology)

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