Synthesis and biologic activities of 11 beta-substituted estradiol as potential antiestrogens.

abstract：:Evaluation of sex steroids in cervical mucus was performed at different phases of spontaneous or clomiphene-citrate-induced ovulatory cycles. To this end, 11 women with normal ovulatory cycles and 9 subjects with polycystic ovary syndrome of comparable age and body mass index were investigated. Serum and cervical mucu...

journal_title：Steroids

authors： Adamopoulos DA,Kapolla N,Abrahamian A,Dessypris A,Nicopoulou S,Giannacodemos G

更新日期：2000-01-01 00:00:00

abstract：:The giant freshwater prawn, Macrobrachium rosenbergii, is important to many Asian countries due to its high economic value as an aquaculture product. With demand increasing, there is requirement for a better understanding of the biosynthetic components that regulate its growth and reproduction, including steroids, in ...

journal_title：Steroids

authors： Thongbuakaew T,Siangcham T,Suwansa-ard S,Elizur A,Cummins SF,Sobhon P,Sretarugsa P

更新日期：2016-03-01 00:00:00

abstract：:The present study was undertaken to examine the mechanism whereby beta-lipotropin stimulates adrenal steroidogenesis. In guinea pig adrenal cells, beta-lipotropin (10(-8) M) increased basal steroid production 6-, 4-, and 5-fold for cortisol, androstenedione, and dehydroepiandrosterone (DHEA), respectively, whereas the...

journal_title：Steroids

authors： O'Connell Y,McKenna TJ,Cunningham SK

更新日期：1996-05-01 00:00:00

abstract：:Two new polyhydroxysteroids isihippurols A (1) and B (2) were isolated from the MeOH extract of the gorgonian Isis hippuris in addition to nine known steroids namely gorgosterol, 3alpha-acetoxy-24-methyl 11beta,18; 18,20beta; 22,25-triepoxy-5alpha-furostane, hippurin-1, 22-epi-hippuristanol, 22-epi-hippurin-1, 3-acety...

journal_title：Steroids

authors： Shen YC,Prakash CV,Chang YT

更新日期：2001-09-01 00:00:00

abstract：:Besides regulating water and electrolyte homeostasis, the mineralocorticoid receptor (MR) elicits pathophysiological effects in the renocardiovascular system. Although the MR's closest relative, the glucocorticoid receptor (GR), acts as a transcription factor at the same hormone-response-element (HRE), activated gluco...

journal_title：Steroids

authors： Grossmann C,Ruhs S,Seiferth A,Gekle M

更新日期：2010-08-01 00:00:00

abstract：:This study examined the role of protein kinase C enzymatic activity as a physiologic determinant of stromal cell death in decidua basalis (DB) during pregnancy. The expression of epidermal growth factor receptor (EGF-R) and Bcl2 was used as an indicator of stromal cell proliferation/survival, whereas Bax and the occur...

journal_title：Steroids

authors： Ogle TF,Dai D,George P

更新日期：1999-09-01 00:00:00

abstract：:Preimplantation rabbit embryos were incubated with pregnenolone and dehydroisoandrosterone under conditions which gave formazan precipitation by the histochemical technique. The metabolic fate of the labeled steroids was assessed simultaneously. There was no concomitant transformation of pregnenolone to progesterone a...

journal_title：Steroids

authors： Bleau G

更新日期：1981-02-01 00:00:00

abstract：:Phytochemical analysis of the fruits of Raphia vinifera led to the isolation of four new steroidal saponins (1-4), along with six known secondary metabolites (6-10). The structures of the isolated compounds were determined based on the analyses of NMR and mass spectrometric data, and chemical degradation reactions. Am...

journal_title：Steroids

authors： Chi GF,Sop RVT,Mbaveng AT,Omollo Ombito J,Fotso GW,Nguenang GS,Kuete V,Efferth T,Ngadjui BT

更新日期：2020-11-01 00:00:00

abstract：:At the development of receptivity the endometrium undergoes specific changes. Several factors have been suggested as markers of endometrial receptivity. A common feature for most of these factors is that they are directly, or indirectly, regulated by progesterone. The effect of various doses and regimens of mifepristo...

journal_title：Steroids

authors： Danielsson KG,Marions L,Bygdeman M

更新日期：2003-11-01 00:00:00

abstract：:This article describes the origins and evolution of "antiestrogenic" medicines for the treatment and prevention of breast cancer. Developing drugs that target the estrogen receptor (ER) either directly (tamoxifen) or indirectly (aromatase inhibitors) has improved the prognosis of breast cancer and significantly advanc...

journal_title：Steroids

authors： Jordan VC,Brodie AM

更新日期：2007-01-01 00:00:00

abstract：:The metabolism of tamoxifen is being redefined in the light of several important pharmacological observations. Recent studies have identified 4-hydroxy N-desmethyltamoxifen (endoxifen) as an important metabolite of tamoxifen necessary for antitumor actions. The metabolite is formed through the enzymatic product of CYP...

journal_title：Steroids

authors： Jordan VC

更新日期：2007-11-01 00:00:00

abstract：:Using a whole cell suspension assay technique, we have examined both the specific binding of testosterone (T) and dihydrotestosterone (17 beta-hydroxy-5 alpha-androstan-3-one) (DHT) and the subsequent distribution of androgen binding activity within MCF-7 human breast cancer cells. We have observed that both androgens...

journal_title：Steroids

authors： MacIndoe JH,Woods GR,Lee FJ

更新日期：1981-10-01 00:00:00

abstract：:Carbenoxolone potentiates the mineralocorticoid activity of endogenous glucocorticoid hormones by inhibiting the enzyme 11 beta-hydroxysteroid dehydrogenase, which converts cortisol and corticosterone to inactive 11-oxo-derivatives. We addressed the question of whether glucocorticoid activity is also affected by carbe...

journal_title：Steroids

authors： Soro A,Panarelli M,Holloway CD,Fraser R,Kenyon CJ

更新日期：1997-04-01 00:00:00

abstract：:MDL 18,962 was shown to be a highly specific, potent (Ki = 3-4 nM), enzyme-activated inhibitor of aromatase with minimal intrinsic endocrine properties. The affinity of MDL 18,962 was higher for human and baboon placental aromatase than for rhesus placental or rodent ovarian aromatase. These species differences necess...

journal_title：Steroids

authors： Johnston JO

更新日期：1987-07-01 00:00:00

abstract：:The formation of a horseradish peroxidase-testosterone conjugate for the enzyme-linked immunoassay of testosterone was investigated, using tritiated testosterone to follow the reaction. The formation of testosterone-3-(carboxymethyl) oxime-peroxidase by the mixed anhydride method was found to give a conjugate of high ...

journal_title：Steroids

authors： Rajkowski KM,Cittanova N,Desfosses B,Jayle MF

更新日期：1977-05-01 00:00:00

abstract：:Several derivatives of the arthropod moulting hormone have been synthesized which were coupled to AH Sepharose 4B yielding about 2 mumole ligand per g wet gel. As an indication of the suitability of the ligands for biological work the puff inducing capacity of their methyl esters was tested. The methyl ester of inokos...

journal_title：Steroids

authors： Spindler KD,Hamann A,Spindler-Barth M,Ihne A,Beckers C,Emmerich H

更新日期：1976-04-01 00:00:00

abstract：:Aspergillus niger, one of fungal species most frequently used for experimental and industrial-scale biotransformations of various organic compounds, is generally known to transform steroids at 16β position. In this work, application of the strain A. niger KCH910 to bioconversion of dehydroepiandrosterone (DHEA), andro...

journal_title：Steroids

authors： Świzdor A,Panek A,Milecka-Tronina N

更新日期：2017-10-01 00:00:00

abstract：:The common disease asthma is characterized by the obstruction, inflammation and increased sensitivity of the airways. Glucocorticoids (GCs) are one of the most potent anti-inflammatory agents available for treating allergic disease. In this study, we report that the GC budesonide (BUD) can rapidly inhibit the histamin...

journal_title：Steroids

authors： Sun HW,Miao CY,Liu L,Zhou J,Su DF,Wang YX,Jiang CL

更新日期：2006-02-01 00:00:00

abstract：:Ischemic heart disease (IHD) continues to be the most common cause of death globally, although mortality rates are decreasing with significant advances in treatment. Higher prevalence of co-morbidities in women only partly explains the lack of decrease in mortality rates in younger women due to. Until recently there h...

journal_title：Steroids

authors： Mihailidou AS,Ashton AW

更新日期：2014-12-01 00:00:00

abstract：:A technique has been developed in which progesterone may be measured by radioimmunoassay in unextracted serum. The method depends on the displacement of progesterone from serum binding proteins by danazol, [17 alpha-pregn-4-en-20-yno (2,3-d) isoxazol-17-ol], a compound which also blocks recombination of free progester...

journal_title：Steroids

authors： McGinley R,Casey JH

更新日期：1979-02-01 00:00:00

abstract：:The 7 alpha-methyl substituent is reported to increase the binding affinity of estradiol for the estrogen receptor (ER). In order to evaluate whether this substituent would improve the in vitro binding characteristics and the in vivo tissue distribution of 18F labeled estrogens that we are developing as positron emiss...

journal_title：Steroids

authors： VanBrocklin HF,Liu A,Welch MJ,O'Neil JP,Katzenellenbogen JA

更新日期：1994-01-01 00:00:00

abstract：:A method for the synthesis and purification of 6beta-iodomethyl-19-norcholest-5(10)-ene-3beta-ol-131I of greater than 98 mole% chemical purity and greater than 99% radiochemical purity is presented. Carbon-13 and proton NMR were used to establish the identity and purity. Discrepancies in the characterization of this c...

journal_title：Steroids

authors： Scott KN,Couch MW,Mareci TH,Williams CM

更新日期：1976-08-01 00:00:00

abstract：:Homogenates from human myometrium with an added NADPH regenerating system and ATP were incubated with 4-(14)C progesterone. Six metabolites were identified: 5alpha-pregnane-3, 20-dione, 5beta-pregnane-3, 20-dione, 3alpha-hydroxy-4-pregnen-20-one, 3beta hydroxy-4-pregnen-20-one. 20alpha-hydroxy-4-pregnen-3-one and 20be...

journal_title：Steroids

authors： Junkermann H,Runnebaum B,Lisboa BP

更新日期：1977-07-01 00:00:00

abstract：BACKGROUND:A high-throughput, sensitive, specific, mass spectrometry-based method for quantitating estrone (E1), estradiol (E2), and testosterone (T) in postmenopausal human serum has been developed for clinical research. The method consumes 100μl human serum for each measurement (triplicates consume 300μl) and does no...

journal_title：Steroids

authors： Wooding KM,Hankin JA,Johnson CA,Chosich JD,Baek SW,Bradford AP,Murphy RC,Santoro N

更新日期：2015-04-01 00:00:00

abstract：:C17-20Lyase and 21-hydroxylase activities were measured during late gestation in the rhesus monkey (Macaca mulatta) fetal adrenal. Activities were assessed in 10,000 x g supernatants with 17-hydroxyprogesterone and NADPH as substrates. Although conversion of [14C]17-hydroxyprogesterone to [14C]androstenedione was note...

journal_title：Steroids

authors： Sholl SA

更新日期：1981-08-01 00:00:00

abstract：:Deltonin is a steroidal saponin which could suppress tumor growth through suppressing angiogenesis, but the mechanisms have not been directly elucidated yet. In the present study, we showed that deltonin inhibited the proliferation of primary cultured human umbilical vein endothelial cells (HUVECs) in vitro; notably, ...

journal_title：Steroids

authors： Tong Q,Zhao Q,Qing Y,Hu X,Jiang L,Wu X

更新日期：2015-04-01 00:00:00

abstract：:Estradiol-17 beta labeled with deuterium in the positions 2 or 4 can be prepared from 2-chloromercurio-1,3,5(10)-estratriene-3,17 beta-diol 3-methyl ether 17-acetate or 4-chloromercurio-1,3,5(10)-estratriene-3,17 beta-diol, respectively, in refluxing CH3COO(2)H/(2)H2O. The same reaction performed on 4-acetoxymercurio-...

journal_title：Steroids

authors： Ferraboschi P,Ravasi M,Santaniello E

更新日期：1983-06-01 00:00:00

abstract：:Although exogenous glucocorticoids (GC) play a role in the regulation of bone marrow mesenchymal stem/stromal cells (MSCs) proliferation and differentiation, the function of endogenous GC is not well understood. The purpose of this study was to investigate the effect of the blockage of endogenous GC using RU486, an an...

journal_title：Steroids

authors： Yu Y,Wei N,Stanford C,Schmidt T,Hong L

更新日期：2012-01-01 00:00:00

abstract：:Estrogen receptor (ER) positive primary breast cancers have a wide range of clinical outcomes. Prediction of the likely course of the disease aids treatment decision-making. In the translational arm of the ATAC (anastrozole or tamoxifen alone or combined) trial (TransATAC) we have assessed individual and multiparamete...

journal_title：Steroids

authors： Dowsett M,Salter J,Zabaglo L,Mallon E,Howell A,Buzdar AU,Forbes J,Pineda S,Cuzick J

更新日期：2011-07-01 00:00:00

abstract：:An efficient method to prepare 5, 9-cyclo-1, 11-oxido-pregn-16-ene-3, 20-dione in one pot was reported. Treatment of 9-bromide-11-hydroxypregna-1, 4, 16-trien-3, 20-dione with Raney Ni in absolute ethanol afforded 5, 9-cyclo-1, 11-oxido-pregn-16-ene-3, 20-dione by two annulation reactions in reasonable yield. The abso...

journal_title：Steroids

authors： Jia P,Wu X,Yu Y,Zhang G

更新日期：2009-02-01 00:00:00