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.
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Authors | Y Nagaoka, T Maeda, Y Kawai, D Nakashima, T Oikawa, K Shimoke, T Ikeuchi, H Kuwajima, S Uesato |
Journal | European journal of medicinal chemistry
(Eur J Med Chem)
Vol. 41
Issue 6
Pg. 697-708
(Jun 2006)
ISSN: 0223-5234 [Print] France |
PMID | 16584813
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Antineoplastic Agents
- Enzyme Inhibitors
- Histone Deacetylase Inhibitors
- Hydroxamic Acids
- ortho-Aminobenzoates
- anthranilamide
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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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