VII. ON THE MECHANISM OF ANTI-ANDROGENIC ACTION OF 16β-ETHYL-17β-HYDROXY-4-OESTREN-3-ONE (TSAA-291)

Autor:	Takuichi Miki, Michio Masuoka, Kentaro Hiraga, Ryo Nakayama
Rok vydání:	1979
Předmět:	medicine.medical_specialty Endocrinology Action (philosophy) Chemistry Endocrinology Diabetes and Metabolism Internal medicine medicine Anti androgenic General Medicine Pharmacology urologic and male genital diseases Mechanism (sociology)
Zdroj:	Acta Endocrinologica. 92:S100-S107
ISSN:	1479-683X 0804-4643
DOI:	10.1530/acta.0.092s100
Popis:	The mechanism of anti-androgenic action of a steroidal compound, TSAA-291, was summarized and discussed in reference to its drug-designing and structure-activity relationship. The target of the drug-design was to obtain a substance which is inactive in androgenic activity and is capable of antagonistically competing with androgen for the receptor. With this intention, the androgen molecule was rendered with a steric hindrance influencing upon the functional 17β-hydroxy group. Introduction of a bulky group at the steroidal position-13 or -16 led to anti-androgenic properties. Intense steric hindrance by introducing an enormously bulky group or complete elimination of the 17β-hydroxy group rather decreased the anti-androgenic activity. Of these anti-androgens thus synthesized, TSAA-291 proved to be the most active in the anti-androgen assay and also antagonistic against the uptake of [3H]testosterone by the rat ventral prostate.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::f0b874aac456e45e3963975c5b71769a https://doi.org/10.1530/acta.0.092s100 Zobrazit plný text záznamu