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Effects of anticancer drugs, metals and antioxidants on cytotoxic activity of benzothiepins/benzoxepins.

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.
AuthorsK Terasawa, H Hosoya, Y Sugita, I Yokoe, H Sakagami
JournalAnticancer research (Anticancer Res) 2000 Sep-Oct Vol. 20 Issue 5A Pg. 2951-4 ISSN: 0250-7005 [Print] Greece
PMID11062706 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents
  • Antioxidants
  • Benzothiepins
  • Benzoxepins
  • Ferric Compounds
  • Metals
  • Copper
  • Doxorubicin
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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