Abstract |
Among 11 benzothiepins/ benzoxepins, 4-chloro-3,4-dihydro-2-(2-oxo-2-phenylethyl)-1-benzothiepin-5-(2H)-one [1] showed the highest cytotoxicity against human oral squamous cell carcinoma HSC-2 cells, followed by 2,3-dihydro-2-(2-oxopropyl)-2-phenyl-1-benzoxepin [2]. Popular antioxidants, such as N-acetyl-L-cysteine and sodium ascorbate significantly reduced the cytotoxic activity of [1] but not that of [2]. Compound [1] induced internucleosomal DNA fragmentation in human promyelocytic leukemic HL-60 cell line, but produced large DNA fragmentation in human oral tumor cell lines (HSC-2, HSG). Compounds [1] and doxorubicin additively reduced the viable cell number of HSC-2 cells. These data, taken together with their tumor specific action, demonstrate for the first time, the medicinal efficacy of benzothiepins/ benzoxepins.
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Authors | K Terasawa, H Hosoya, Y Sugita, I Yokoe, H Sakagami |
Journal | Anticancer research
(Anticancer Res)
2000 Sep-Oct
Vol. 20
Issue 5A
Pg. 2951-4
ISSN: 0250-7005 [Print] Greece |
PMID | 11062706
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Antineoplastic Agents
- Antioxidants
- Benzothiepins
- Benzoxepins
- Ferric Compounds
- Metals
- Copper
- Doxorubicin
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Topics |
- Antineoplastic Agents
(pharmacology)
- Antioxidants
(pharmacology)
- Apoptosis
(drug effects)
- Benzothiepins
(chemistry, pharmacology)
- Benzoxepins
(chemistry, pharmacology)
- Carcinoma, Squamous Cell
- Cell Survival
(drug effects)
- Copper
- DNA Fragmentation
(drug effects)
- Doxorubicin
(pharmacology)
- Drug Synergism
- Ferric Compounds
- HL-60 Cells
- Humans
- Metals
- Molecular Structure
- Mouth Neoplasms
- Salivary Gland Neoplasms
- Tumor Cells, Cultured
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