Compounds > 3-(4-5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2h-tetrazolium

3-(4-5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2h-tetrazolium and hydroxyflutamide

3-(4-5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2h-tetrazolium has been researched along with hydroxyflutamide* in 1 studies

Other Studies

1 other study(ies) available for 3-(4-5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2h-tetrazolium and hydroxyflutamide

Article	Year
Non-steroidal L-245,976 acts as a classical antiandrogen in vitro. The Journal of steroid biochemistry and molecular biology, 1997, Volume: 60, Issue:1-2 Non-steroidal antiandrogens have been employed in the management of prostate cancer, but the mechanism of action is unclear due to a lack of good tissue culture models. The growth of a hamster ductus deferens cell line (DDT1) is highly dependent upon the addition of 10 nM testosterone to synthetic serum-free media. We describe a non-steroidal compound N-(4-chlorophenyl)-(Z,Z)-2,3-bis(-cyclopropylmethylene) cyclopentanecarboxamide (L-245976) which antagonizes the action of testosterone on DDT1 cells at 10 microM but exhibits little or no effect on cell growth by itself. This compound also blocks the binding of 3H-dihydrotestosterone (DHT) to the human androgen receptor (AR) with an IC50 of approximately 28 microM. In addition, L-245976 was found to antagonize DHT-dependent transactivation of the AR via the probasin gene promoter at comparable doses with no agonist activity. Topics: Amides; Androgen Antagonists; Androgen-Binding Protein; Androgens; Aniline Compounds; Animals; Cell Division; Cell Line; CHO Cells; Colorimetry; Cricetinae; Dihydrotestosterone; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; Flutamide; Formazans; Humans; Male; Receptors, Androgen; Recombinant Proteins; Testosterone; Tetrazolium Salts; Thiazoles; Transcriptional Activation; Transfection; Vas Deferens	1997

Article

Year

Non-steroidal L-245,976 acts as a classical antiandrogen in vitro.

The Journal of steroid biochemistry and molecular biology, 1997, Volume: 60, Issue:1-2

Non-steroidal antiandrogens have been employed in the management of prostate cancer, but the mechanism of action is unclear due to a lack of good tissue culture models. The growth of a hamster ductus deferens cell line (DDT1) is highly dependent upon the addition of 10 nM testosterone to synthetic serum-free media. We describe a non-steroidal compound N-(4-chlorophenyl)-(Z,Z)-2,3-bis(-cyclopropylmethylene) cyclopentanecarboxamide (L-245976) which antagonizes the action of testosterone on DDT1 cells at 10 microM but exhibits little or no effect on cell growth by itself. This compound also blocks the binding of 3H-dihydrotestosterone (DHT) to the human androgen receptor (AR) with an IC50 of approximately 28 microM. In addition, L-245976 was found to antagonize DHT-dependent transactivation of the AR via the probasin gene promoter at comparable doses with no agonist activity.

Topics: Amides; Androgen Antagonists; Androgen-Binding Protein; Androgens; Aniline Compounds; Animals; Cell Division; Cell Line; CHO Cells; Colorimetry; Cricetinae; Dihydrotestosterone; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; Flutamide; Formazans; Humans; Male; Receptors, Androgen; Recombinant Proteins; Testosterone; Tetrazolium Salts; Thiazoles; Transcriptional Activation; Transfection; Vas Deferens

1997