Synthesis and biological evaluation of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitors based on a thieno[2,3-d]pyrimidin-4(3H)-one core.

Many breast tumors are hormone-dependent, and estrogens, especially estradiol (E2), have a pivotal role in their growth and development. 17beta-Hydroxysteroid dehydrogenase type 1 (17beta-HSD1) is a key enzyme in the biosynthesis of female sex steroids, catalyzing the NADPH-dependent reduction of estrone into biologically active estradiol. In this study, a library of fused (di)cycloalkeno thieno[2,3-d]pyrimidin-4(3H)-one based compounds was synthesized, and the biological activities against 17beta-HSD1 in a cell-free and in a cell-based assay were evaluated.

Regulation of ovarian UT-OC-2 carcinoma cells by cytokines: effects on cell proliferation, activation of transcription factors and apoptosis.

Background: It is known that immunologic factors are involved in the regulation of the growth of ovarian carcinoma and that granulocytes are often found on the site of ovarian cancer. Therefore, we chose to investigate the effects of cytokines on UT-OC-2 ovarian endometrioid adenocarcinoma cells in vitro. In order to investigate the molecular mechanisms involved, the activation of two key DNA-binding proteins, AP-1 and transcription factor NF-kappaB (NF-kappaB), was studied.

Effects of ospemifene and raloxifene on hormonal status, lipids, genital tract, and tolerability in postmenopausal women.

Objective: To compare ospemifene and raloxifene regarding their effects on hormones, lipids, genital tract, and tolerability in postmenopausal women.

Design: A randomized, double-blind study in which 118 healthy postmenopausal women received 30 (n = 29), 60 (n = 30), or 90 mg (n = 30) of ospemifene or 60 mg (n = 29) of raloxifene for 3 months.

Results: There were no significant differences in the baseline characteristics between study groups.

Activin B in patients with granulosa cell tumors: serum levels in comparison to inhibin.

Background: Activins and inhibins are polypeptide hormones/growth factors of primarily gonadal origin. In the ovary, activins and inhibins are primarily synthesized by granulosa cells. Serum inhibin measurements have been used for the follow-up of patients with granulosa-cell tumors (GCT) after surgery.

Endometrial thermoablation for treatment of menorrhagia: comparison of two methods in outpatient setting.

Background: Menorrhagia is one of the commonest reasons for gynecologic consultations. Inhibitors of fibrinolysis and non-steroidal anti-inflammatory drugs (NSAIDs) are generally used as therapy for the condition with an acceptable response in some patients. Endometrial ablation is one choice in patients suffering from menorrhagia.