Biotransformation and molecular docking studies of aromatase inhibitors.

abstract：:The preparation of ring-A fused pyrimidines at the steroidal 2,3-position is herein described. The novel steroidal pyrimidines were prepared from the solid phase three-component reaction of 2-hydroxymethylene-3-keto steroids, arylaldehydes and ammonium acetate under microwave irradiation. ...

journal_title：Steroids

authors： Barthakur MG,Gogoi S,Dutta M,Boruah RC

更新日期：2009-09-01 00:00:00

abstract：:Some properties of immunoreactive estradiol secreted by adrenals and ovaries of immature female rats were studied. It was shown that adrenals and ovaries of 15-day-old animals secrete approximately equal amounts of immunoreactive estradiol, with thin-layer chromatogram of immunoreactive material being identical for bo...

journal_title：Steroids

authors： Tinnikov AA,Bazhan NM,Yakovleva TV

更新日期：1992-04-01 00:00:00

abstract：:Allopregnanolone (3α-THP) is one of the main reduced progesterone (P4) metabolites that is recognized as a neuroprotective and myelinating agent. 3α-THP also induces proliferation of different neural cells. It has been shown that P4 favors the progression of glioblastomas (GBM), the most common and aggressive primary ...

journal_title：Steroids

authors： Zamora-Sánchez CJ,Hansberg-Pastor V,Salido-Guadarrama I,Rodríguez-Dorantes M,Camacho-Arroyo I

更新日期：2017-03-01 00:00:00

abstract：:Glucocorticoids are an important class of anti-inflammatory/immunosuppressive drugs. A crucial part of their anti-inflammatory action results from their ability to repress proinflammatory transcription factors such as nuclear factor-κB (NF-κB) and activator protein-1 (AP-1) upon binding to the glucocorticoid receptor ...

journal_title：Steroids

authors： Cechin SR,Buchwald P

更新日期：2014-07-01 00:00:00

abstract：:Within the adult female, estrogen signaling is well-described as an integral component of the physiologically significant hypothalamic-pituitary-gonadal axis. In rodents, the timing of ovulation is intrinsically entwined with the display of sexual receptivity. For decades, the importance of estradiol activating intrac...

journal_title：Steroids

authors： Tonn Eisinger KR,Larson EB,Boulware MI,Thomas MJ,Mermelstein PG

更新日期：2018-05-01 00:00:00

abstract：:A technique of incubation of testicular tissue in vitro with radiolabeled precursors was applied in the investigation of the steroid biosynthesis by testes of four young men after long-term, high-dose estrogen treatment. A positive correlation between plasma and testicular steroid levels, and in vitro capacity of the ...

journal_title：Steroids

authors： Rodriguez-Rigau LJ,Tcholakian RK,Smith KD,Steinberger E

更新日期：1977-06-01 00:00:00

abstract：:Preparative chemical methods for the synthesis of eight oxidative transformation products of ethinyl estradiol (EE) and norethindrone acetate (NA) are described. The prepared materials are useful as reference materials and standards for pharmaceutical analysis of EE and NA as bulk chemical or in formulated product. Al...

journal_title：Steroids

authors： Ekhato IV,Hurley T,Lovdahl M,Revitte TJ,Guo L,Huang Y,Clipper S,Colson C

更新日期：2002-03-01 00:00:00

abstract：:The preparation of 3-oxo-4-azasteroid from A-nor-3,5-secosteroid-3-oic acid is described in a solventless condition catalysed by Lewis acid under microwave irradiation. We utilized urea as an environmentally benign source for the generation of ammonia for the aza cyclization reaction. ...

journal_title：Steroids

authors： Borthakur M,Boruah RC

更新日期：2008-07-01 00:00:00

abstract：:In our effort to develop imaging agents for brain glucocorticoid receptors, we have prepared several novel glucocorticoids possessing a 2-methylsulfanyl-acetyl side chain. The synthesis was accomplished via a Mitsunobu reaction with thiobenzoic acid starting from cortisol, prednisolone, dexamethasone and triamcinolone...

journal_title：Steroids

authors： Wuest F,Carlson KE,Katzenellenbogen JA

更新日期：2008-01-01 00:00:00

abstract：:These studies investigated whether treatment with carbenoxolone (CBX), an inhibitor of 11 beta-hydroxysteroid dehydrogenase (11 beta-HSD), resulted in an enhanced mineralocorticoid response to endogenous or infused cortisol. In conscious sodium replete sheep with a parotid fistula, infusion of CBX (40 mg/h for 10 days...

journal_title：Steroids

authors： Dodic M,May CN,Coghlan JP

更新日期：1998-02-01 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：:Inhibition of 5alpha-reduction of testosterone by an anti-androgen TSAA-291 (16beta-ethyl-17beta-hydroxy-4-estren-3-one) was studied in rat ventral prostates and the metabolic conversion of 3H-TSAA-291 was examined both in vitro and in vivo. In the in vitro experiment using nuclear 5alpha-reductase of the prostate, 5a...

journal_title：Steroids

authors： Sudo K,Yoshida K,Akinaga Y,Nakayama R

更新日期：1981-07-01 00:00:00

abstract：:Fast atom bombardment/mass spectrometry or liquid secondary ion mass spectrometry provides the capability for direct analysis of steroid conjugates (sulfates, glucuronides) without prior hydrolysis or derivatization. During the analysis of biologic extracts, limitations on the sensitivity of detection arise from the p...

journal_title：Steroids

authors： Gaskell SJ

更新日期：1990-10-01 00:00:00

abstract：:Incubation of aldosterone with confluent layers of A6 (toad kidney) cells leads to its hydroxylation at the 6 beta-position. 6 beta-Hydroxyaldosterone is the major metabolite when the incubation is carried out at pH 6.8, whereas the product comprises 6 beta-hydroxy-17-isoaldosterone accompanied by some 6 beta-hydroxya...

journal_title：Steroids

authors： Morris DJ,Latif SA,Conca TJ,Wei LT,Watlington CO,Kirk DN,Toms HC,Shackleton CH

更新日期：1990-11-01 00:00:00

abstract：OBJECTIVE:To evaluate the role of physiologic levels of androgens and their precursors in the regulation of body composition, energy and substrate metabolism and aerobic capacity in healthy, cycling, premenopausal women. EXPERIMENTAL:We evaluated 30 young (27±1 year) premenopausal, non-obese (23±0.5 kg/m(2)), normally...

journal_title：Steroids

authors： Keller JL,Casson PR,Toth MJ

更新日期：2011-11-01 00:00:00

abstract：:The apolar ecdysteroid present in the developing embryo of the blue crab, Callinectes sapidus Rathbun, is tentatively identified as ponasterone A (2 beta, 14 alpha, 20,22-pentahydroxy-5, beta-cholest-7-en-6-one) on the basis of chromatographic, immunological, and mass spectral evidence. The apolar ecdysteroid present ...

journal_title：Steroids

authors： McCarthy JF

更新日期：1979-12-01 00:00:00

abstract：:A radioimmunoassay of three deoxycorticoids, namely 11 beta,17 alpha-dihydroxy-4-pregnene-3,20-dione (21-deoxycortisol), 17 alpha,21-dihydroxy-4-pregnene-3,20-dione (11-deoxycortisol), and 21-hydroxy-4-pregnene-3,20-dione (11-deoxycorticosterone) which are important for differential diagnosis of congenital adrenal dis...

journal_title：Steroids

authors： Hill M,Lapcík O,Hampl R,Stárka L,Putz Z

更新日期：1995-09-01 00:00:00

abstract：BACKGROUND AND AIMS:Calcitriol, an active vitamin D metabolite, has a limited application in bone repair because of its undesirable hypercalcaemic action. However it has emerged that lithocholic acid (LCA) is a non-calcaemic vitamin D receptor ligand but whether this steroid can support osteoblast maturation has not be...

journal_title：Steroids

authors： Mansell JP,Shorez D,Farrar D,Nowghani M

更新日期：2009-11-01 00:00:00

abstract：:Endochondral bone formation is a precise and highly ordered process whose exact regulatory framework is still being elucidated. Multiple regulatory pathways are known to be involved. In some cases, regulation impacts gene expression, resulting in changes in chondrocyte phenotypic expression and extracellular matrix sy...

journal_title：Steroids

authors： Asmussen N,Lin Z,McClure MJ,Schwartz Z,Boyan BD

更新日期：2019-02-01 00:00:00

abstract：:The non-genomic action of steroid hormones regulates a wide variety of cellular responses including regulation of ion transport, cell proliferation, migration, death and differentiation. In order to achieve such plethora of effects steroid hormones utilize nearly all known signal transduction pathways. One of the key ...

journal_title：Steroids

authors： Alzamora R,Harvey BJ

更新日期：2008-10-01 00:00:00

abstract：:The mode of action of steroid hormones has been extended in recent years. In addition to their classical nuclear action (acting as transcription factors), they can also regulate cell-signaling phosphorylation cascades and exert actions that are initiated at the membrane and which, in most cases, are rapid. Even though...

journal_title：Steroids

authors： Kampa M,Pelekanou V,Castanas E

更新日期：2008-10-01 00:00:00

abstract：:To investigate the effects of conjugated bile acid on bacterial growth and cholylglycine hydrolase activity, Clostridium perfringens from human feces was exposed to varying concentrations of taurine- or glycine-conjugated chenodeoxycholic acid. Extracellular enzyme activity was determined by deconjugation of radiolabe...

journal_title：Steroids

authors： Kishinaka M,Umeda A,Kuroki S

更新日期：1994-08-01 00:00:00

abstract：:Prostaglandin E(2) (PGE(2)) is a major mediator in the pathophysiology, and pathogenesis of gynecological diseases associated with abnormal endometrial disease with proliferation and inflammation, such as endometriosis. In this study, we investigated the effect of dienogest, a selective progesterone receptor agonist, ...

journal_title：Steroids

authors： Shimizu Y,Mita S,Takeuchi T,Notsu T,Mizuguchi K,Kyo S

更新日期：2011-01-01 00:00:00

abstract：:Dehydroepiandrosterone (DHEA) reduces body fat in rodents and humans, and increases glycerol release from isolated rat epididymal adipocytes and human visceral adipose tissue explants. It suggests that DHEA stimulates triglyceride hydrolysis in adipose tissue; however, the mechanisms underlying this action are still u...

journal_title：Steroids

authors： Karbowska J,Kochan Z

更新日期：2012-11-01 00:00:00

abstract：:The hepatic metabolism of 3-oxoandrost-4-ene-17 beta-carboxylic acid (etienic acid), a probable acidic catabolite of deoxycorticosterone, was investigated using rats prepared with an external biliary fistula. Metabolic products were identified by GC-MS after hydrolysis with beta-glucuronidase and by proton nuclear mag...

journal_title：Steroids

authors： Radominska A,Little JM,Lester R,St Pyrek J

更新日期：1992-07-01 00:00:00

abstract：:Two new 4-methyl-progesteroids, nodulisporisteriod A (1) and nodulisporisteriod B (2), were isolated from the extract of an endolichenic fungal strain Nodulisporium sp. (No. 65-17-2-1), along with two related metabolites, demethoxyviridin (3) and inoterpene B (4). Their structures were determined by detailed spectrosc...

journal_title：Steroids

authors： Zheng QC,Chen GD,Kong MZ,Li GQ,Cui JY,Li XX,Wu ZY,Guo LD,Cen YZ,Zheng YZ,Gao H

更新日期：2013-09-01 00:00:00

abstract：:A sensitive accurate assay for the placental microsomal 3 beta-hydroxysteroid dehydrogenase (E.C.1.1.1.51) has been developed using tritiated substrates. Kinetic analysis of the enzyme with 3 beta-hydroxy-5-androsten-17-one and 3 beta-hydroxy-5-pregnen-20-one indicates that the apparent Km values for these substrates ...

journal_title：Steroids

authors： Gibb W

更新日期：1979-04-01 00:00:00

abstract：:Structural transformation of the steroidal lactone, oxandrolone (1), by suspended-cell cultures of the plant pathogen fungus Rhizopus stolonifer, resulted in the production of three new metabolites. These metabolites were identified as 11alpha-hydroxyoxandrolone (2), 6alpha-hydroxyoxandrolone (3) and 9alpha-hydroxyoxa...

journal_title：Steroids

authors： Choudhary MI,Mohammad MY,Musharraf SG,Parvez M,Al-Aboudi A,Atta-ur-Rahman

更新日期：2009-11-01 00:00:00

abstract：:Orally administered testosterone undecanoate (TU), an anabolic, androgenic steroid, can potentially be abused by athletes. Indirect evidence for detecting oral TU intake could be deduced from the changes in steroid profile post-administration. Direct evidence could be obtained by detection of unchanged TU in plasma. T...

journal_title：Steroids

authors： Peng SH,Segura J,Farré M,González JC,de la Torre X

更新日期：2002-01-01 00:00:00

abstract：:A number of progesterone derivatives, having a 17 alpha-acetoxy group and various functions at C-3 and C-6, interact at the cardiac glycoside (CG) binding site, using [3H]ouabain in a radioligand binding assay (RBA) with membranes from dog myocardium. We now report on results of structure-activity studies concerned wi...

journal_title：Steroids

authors： Templeton JF,Kumar VP,Kim RS,LaBella FS

更新日期：1987-04-01 00:00:00