A chemical classification of nonsteroidal antagonists of sex-steroid hormone action.
A highly varied collection of nonsteroids have been reported over the last forty years as being able to exert an antihormonal action versus steroid hormones in vivo. This diversity is partly explained by the manifold molecular targets of these compounds which may be either enzymes or receptors (leading to inhibition of steroid production and action respectively) and by the different possible levels of interference within feedback loops between the central nervous system, pituitary, gonads and other peripheral organs. The present chapter is a chemist's classification of some of these structures often in the absence of detailed biochemical data. Nonsteroid antiestrogens (and estrogens) most often share a common feature with diethylstilbestrol and consequently the effects of structural modifications on biological activities can be studied in a rational manner. This is not the case for non-steroidal antiandrogens that we have only been able to classify into conventional chemical groups. Nor have any true lead compounds nor well-defined chemical classes been identified for nonsteroid antiprogestogens. This is however the only hormonal class where natural products play an important role.
Miquel
J F
JF
Centre d'Etudes et de Recherches de Chimie Organique Appliquée (CERCOA)-C.N.R.S., Thiais, France.
Gilbert
J
J
D000726:Androgen Antagonists; D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D004965:Estrogen Antagonists; D012739:Gonadal Steroid Hormones / Q000037:antagonists & inhibitors*; D006801:Humans; D011372:Progestins / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship
D000726:Androgen Antagonists; D004965:Estrogen Antagonists; D012739:Gonadal Steroid Hormones; D011372:Progestins