Abstract
The aim of the study was to find new antiestrogenic and antiandrogenic structures. Out of the triphenyl-alkene derivatives Panomifene (EGIS-5660) proved to be the most active antiestrogenic compound which binds to specific estrogen receptors and exhibits inhibitory effects on experimental mammary tumors both in vitro and in vivo. The investigated antiandrogenic compounds were indol and imidazole derivatives. One of these compounds a di-imidazolil derivative, GYK1-24479 inhibited the in vitro androgen (testosterone and androstenedione) biosynthesis both in vitro and in vivo in concentration/dose dependent manner, and in these respects proved to be more active than the referent ketoconazole.
MeSH terms
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Androgen Antagonists / metabolism
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Androgen Antagonists / pharmacology*
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Androgens / blood
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Animals
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Antineoplastic Agents, Hormonal / metabolism
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Antineoplastic Agents, Hormonal / pharmacology*
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Breast Neoplasms / drug therapy
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Corticosterone / blood
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Estrogen Antagonists / metabolism
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Estrogen Antagonists / pharmacology*
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Female
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Humans
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Imidazoles / pharmacology*
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In Vitro Techniques
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Mammary Neoplasms, Experimental / chemically induced
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Mammary Neoplasms, Experimental / prevention & control
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Rats
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Receptors, Estrogen / antagonists & inhibitors
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Tamoxifen / analogs & derivatives*
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Tamoxifen / metabolism
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Tamoxifen / pharmacology
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Tumor Cells, Cultured
Substances
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Androgen Antagonists
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Androgens
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Antineoplastic Agents, Hormonal
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Estrogen Antagonists
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GYKI 24479
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Imidazoles
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Receptors, Estrogen
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Tamoxifen
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panomifene
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Corticosterone