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Beschreibung

A cell-permeable benzylidine-thioxothiazolidinone compound that blocks the steroidogenesis of testosterone by directly inhibiting 17&beta,-HSD3- (17&beta,-hydroxysteroid dehydrogenase type 3) catalyzed, NADPH-dependent, reduction of &Delta,4-dione C17 ketone in a &Delta,4-dione- (4-androstene-3,17-dione) competitive, highly potent (IC50 = 0.6, 6.0, and 40 nM, respectively, against momoset, human, and mouse 17&beta,-HSD3 activity in testes homogenate), and selective manner, displaying no activity against 17&beta,-HSD1 and 17&beta,-HSD2 activity. Poor pharmacokinetic properties limit its use to culture treatments and cell-free assays only., A cell-permeable benzylidine-thioxothiazolidinone compound that blocks the steroidogenesis of the potent androgen testosterone by directly inhibiting 17&beta,-HSD3- (17&beta,-hydroxysteroid dehydrogenase type 3) catalyzed, NADPH-dependent, reduction of &Delta,4-dione C17 ketone in a &Delta,4-dione- (4-androstene-3,17-dione) competitive, highly potent (IC50 = 0.6, 6.0, and 40 nM, respectively, against momoset, human, and mouse 17&beta,-HSD3 activity in testes homogenate, IC50 = 14 nM using 17&beta, HSD3-transfected HeLa cells), and selective manner, displaying no activity against 17&beta,-HSD1 and 17&beta,-HSD2 activity in HeLa transfectants or AR- (andogen receptor), ER&alpha,- (estrogen receptor &alpha,), and GR- (glucocorticoid receptor) dependent transcription activities. Low aqueous solubility, lack of oral availability, and other poor pharmacokinetic properties limit its use to culture treatments and cell-free assays only.