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Solid-Phase Organic Synthesis (SPOS) of Modulators of Estrogenic and Androgenic Action

[ Vol. 6 , Issue. 1 ]


Donald Poirier and Rene Maltais   Pages 37 - 52 ( 16 )


Estrogens and androgens are key growing factors involved in a large series of disorders. Two main strategies are possible for controlling their undesirable agonist effects: (1) blocking their biosynthesis by using selective enzyme inhibitors, and (2) antagonizing their hormonal action on a receptor with an antiestrogen or an antiandrogen. In this review, we will briefly discuss the identification of a series of important therapeutic targets, through the study of steroidogenesis of potent estrogens, estrone and estradiol, and potent androgens, testosterone and dihydrotestosterone, as well as of their nuclear receptors. We will next review the solid-phase synthesis of steroidogenic enzyme (steroid sulfatase and 17β-hydroxysteroid dehydrogenases) inhibitors and steroid (estrogen and androgen) receptor modulators, all being potential therapeutic agents for the treatment of hormone-sensitive diseases.


Sulfotransferase, hydroxysteroids, polymer-bound glycerol, diversification, nuclear estrogen receptors, acylation


Medicinal Chemistry Division, Oncology and Molecular Endocrinology Research Center, CHUQ-Pavillon CHUL, 2705 Boulevard Laurier, QuEbec, Qc, G1V 4G2, Canada.

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