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Influence of 2-(4-aminophenyl)benzothiazoles on growth of human ovarian carcinoma cells in vitro and in vivo.
- Source :
-
British journal of cancer [Br J Cancer] 1998 Aug; Vol. 78 (4), pp. 421-9. - Publication Year :
- 1998
-
Abstract
- 2-(4-Aminophenyl)benzothiazole molecules substituted in the 3 position of the phenyl ring with a halogen atom or methyl moiety comprise a group of compounds that potently inhibit specific human ovarian carcinoma cell lines. GI50 values fall within the nM range. Inhibition is highly selective -- whereas the GI50 value in IGROV1 cells consistently lies at < 10 nM, SK-OV-3 presents GI50 values > 10 microM. Biphasic dose-response relationships were observed in sensitive cell lines after 48-h drug exposure. COMPARE analyses revealed the very similar profiles of anti-tumour activity of 3-substituted benzothiazoles and 5-(4-dimethylaminophenylazo)quinoline, with Pearson correlation coefficients > 0.65. Anti-tumour activity extended to preliminary in vivo tests. The growth of OVCAR-3 cells in polyvinylidene fluoride (PVDF) hollow fibres implanted in the peritoneal cavity of mice was inhibited by more than 50% after intraperitoneal (i.p.) administration of 2-(4-amino-3-methylphenyl)benzothiazole (10 mg kg(-1)), 2-(4-amino-3-chlorophenyl)benzothiazole (100 mg kg(-1)) or 2-(4-amino-3-bromophenyl)benzothiazole (150 mg kg(-1)). The growth of OVCAR-3 tumours in subcutaneously (s.c.) implanted hollow fibres was retarded by more than 50% after treatment with 2-(4-amino-3-methylphenyl)benzothiazole (6.7 and 10 mg kg(-1)). In addition, the growth of s.c. OVCAR-3 xenografts was delayed after exposure to DF 203. However, the relationship between drug concentration and growth inhibition was inverse.
- Subjects :
- Animals
Antineoplastic Agents pharmacology
Benzothiazoles
Cell Division drug effects
Dose-Response Relationship, Drug
Female
Humans
Mice
Mice, Nude
Neoplasm Transplantation
Thiazoles pharmacology
Transplantation, Heterologous
Tumor Cells, Cultured
Antineoplastic Agents therapeutic use
Ovarian Neoplasms drug therapy
Thiazoles therapeutic use
Subjects
Details
- Language :
- English
- ISSN :
- 0007-0920
- Volume :
- 78
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- British journal of cancer
- Publication Type :
- Academic Journal
- Accession number :
- 9716022
- Full Text :
- https://doi.org/10.1038/bjc.1998.510