Synthesis, NMR and crystal characterization of dimeric terephthalates derived from epimeric 4,5-seco-cholest-3-yn-5-ols.

abstract：:The 1,3-dipolar cycloaddition of azomethine ylide derived in situ from the reaction of acenaphthylene-1,2-dione and 1,3-thiazolane-4-carboxylic acid to various exocyclic dipolarophiles synthesized from trans-androsterone and trans-dehydroandrosterone afforded a library of novel spiro[5'.2″]acenaphthylene-1″-one-spiro[...

journal_title：Steroids

authors： Kanchithalaivan S,Kumar RR,Perumal S

更新日期：2013-04-01 00:00:00

abstract：:Dehydroepiandrosterone (DHEA) is a multifunctional steroid with a broad range of biological effects in humans and animals. DHEA can be converted to multiple oxygenated metabolites in the brain and peripheral tissues. The mechanisms by which DHEA exerts its effects are not well understood. However, evidence that the ef...

journal_title：Steroids

authors： El Kihel L

更新日期：2012-01-01 00:00:00

abstract：:Human keratinocytes convert 25(OH)D(3) to hormonally active 1alpha,25(OH)(2)D(3) and respond to its antiproliferative/prodifferentiating action in vitro and in vivo. Levels and activity of 1alpha,25(OH)(2)D(3) are short-lived. 1alpha,25(OH)(2)D(3) induces 24-hydroxylase (CYP24) that rapidly metabolizes the hormone, yi...

journal_title：Steroids

authors： Schuster I,Egger H,Bikle D,Herzig G,Reddy GS,Stuetz A,Stuetz P,Vorisek G

更新日期：2001-03-01 00:00:00

abstract：:The synthesis of 16 alpha-3H androgens and estrogens is described. 1-(3H)-Acetic acid in the presence of zinc dust reacts with 16 alpha-bromo-17-ketosteroids to produce 16 alpha-3H-17-ketosteroids. This chemical reaction was used to prepare 16 alpha-3H-dehydroepiandrosterone (I) and 16 alpha-3H-estrone acetate (XI) fr...

journal_title：Steroids

authors： Cantineau R,Kremers P,De Graeve J,Cornelis A,Laszlo P,Gielen JE,Lambotte R

更新日期：1981-02-01 00:00:00

abstract：:In this study, we assessed the rate of estradiol degradation via the 17 beta-hydroxysteroid dehydrogenase (HSD) enzyme in breast tumors from postmenopausal women. We initially studied the effects of time, level of enzyme activity, amount of tissue assayed, and substrate concentration on the linearity of conversion of ...

journal_title：Steroids

authors： Leszczynski D,Santner SJ,Feil PD,Santen RJ

更新日期：1988-03-01 00:00:00

abstract：:Synthesis of 7-aryl/allyl-substituted androstene derivatives 3a through 3g has been carried out by Grignard reaction on 3 beta,17 beta-diacetoxyandrost-5-en-7-one (2) with aryl/allyl magnesium bromide. Isomeric mixture of products 3b and 3c/3e and 3f/3h was separated by column chromatography. Stereochemical assignment...

journal_title：Steroids

authors： Grover A,Dwivedy I,Singh AK,Ray S,Singh MM,Kamboj VP

更新日期：1991-09-01 00:00:00

abstract：OBJECTIVE:The cut-off value for salivary cortisol measurement for the diagnosis of Cushing's syndrome (CS) may depend both on the severity of the disease and the composition of control group. Therefore, we examined the utility of midnight salivary cortisol measurements in patients who were evaluated for signs and sympt...

journal_title：Steroids

authors： Sereg M,Toke J,Patócs A,Varga I,Igaz P,Szücs N,Horányi J,Pusztai P,Czirják S,Gláz E,Rácz K,Tóth M

更新日期：2011-01-01 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：:Ten sex steroids were measured in the peripheral serum and ovarian follicular fluid of female pigs with or without cystic ovarian disease. In general, progestin, especially progesterone, accumulated excessively in the fluid contained in cystic compared with normal follicles. Nonluteinized cystic follicles contained up...

journal_title：Steroids

authors： Babalola GO,Shapiro BH

更新日期：1990-07-01 00:00:00

abstract：:Using dehydroepiandrosterone as the starting material, we have synthesized a series of steroid analogs possessing a D-ring fused with heterocycles which are pyridine, imidazo [2,1-b]thiazoles or substituted thiazole imines. All the final structures are first reported and identified by NMR and MS spectroscopys, the yie...

journal_title：Steroids

authors： Zhang BL,Zhang E,Pang LP,Song LX,Li YF,Yu B,Liu HM

更新日期：2013-12-11 00:00:00

abstract：:A convenient procedure for the synthesis of 5 beta-cholestane-3 alpha,7 alpha,12 alpha,25-tetrol via a modified homologation sequence of the intermediate 3 alpha,7 alpha,12 alpha-triformyloxy-24-oxo-25-diazo-25-homo-5 beta-cholane involving a homogeneous medium is described. This involves treating the intermediate alp...

journal_title：Steroids

authors： Dayal B,Bagan E,Speck J,Salen G

更新日期：1980-04-01 00:00:00

abstract：BACKGROUND:Congenital adrenal hyperplasia (CAH) caused by 21-hydroxylase deficiency (21OHD) is an autosomal recessive disorder due to mutation in the CYP21A2 gene. OBJECTIVE:To elucidate the genetic basis of 21-hydroxylase-deficient CAH in Hong Kong Chinese patients. PATIENTS AND METHODS:Mutational analysis of the CY...

journal_title：Steroids

authors： Chan AO,But WM,Ng KL,Wong LM,Lam YY,Tiu SC,Lee KF,Lee CY,Loung PY,Berry IR,Brown R,Charlton R,Cheng CW,Ho YC,Tse WY,Shek CC

更新日期：2011-09-01 00:00:00

abstract：:A partial synthesis of the title compound, 4'-(dimethylamino)-17 beta-hydroxy-17 alpha-(1-propynyl)benzo[12,12a]-11 alpha,18-cyclo-12a,12b- dihomo-13 alpha-estr-4-en-3-one 1, is reported. The key step in this synthesis represents an intramolecular alkenylaryl radical cyclization. Treatment of 18-[bromo-5-(dimethylamin...

journal_title：Steroids

authors： Ottow E,Beier S,Elger W,Fritzemeier KH,Neef G,Wiechert R

更新日期：1994-03-01 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：:Glucuronidation of 24,25-dihydroxyvitamin D3 has been investigated in in vitro and in vivo experiments. Three positional isomers of 24,25-dihydroxyvitamin D3 monoglucuronide were synthesized from 24,25-dihydroxyprovitamin D3 derivatives with Koenigs-Knorr reaction and used as standard samples. In the presence of the r...

journal_title：Steroids

authors： Higashi T,Horike M,Kikuchi R,Shimada K

更新日期：1999-10-01 00:00:00

abstract：:Lung cancer is the most common cause of cancer mortality in male and female patients in the US. The etiology of non-small cell lung cancer (NSCLC) is not fully defined, but new data suggest that estrogens and growth factors promote tumor progression. In this work, we confirm that estrogen receptors (ER), both ERalpha ...

journal_title：Steroids

authors： Márquez-Garbán DC,Chen HW,Fishbein MC,Goodglick L,Pietras RJ

更新日期：2007-02-01 00:00:00

abstract：:Three BS-BODIPY (brassinosteroids-4,4-difluoro-4-bora-3a,4a-diaza-s-indacene) conjugates were synthesized and their fluorescent and immunological properties were investigated. Two of the conjugates, having present all the functional groups characteristic of BS, were shown to be potentially useful as biological probes ...

journal_title：Steroids

authors： Malachowska-Ugarte M,Sperduto C,Ermolovich YV,Sauchuk AL,Jurášek M,Litvinovskaya RP,Straltsova D,Smolich I,Zhabinskii VN,Drašar P,Demidchik V,Khripach VA

更新日期：2015-10-01 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：:The first natural occurrence of 19-norcholestenone is reported, together with 17 sterols and one other delta 4-3-ketone in the extracts of the Californian gorgonian, Muricea californica (Aurivillius). Six additional demethyl sterols and five additional 4-monomethyl sterols which remain unidentified were also detected....

journal_title：Steroids

authors： Popov S,Carlson RM,Djerassi C

更新日期：1983-04-01 00:00:00

abstract：:The binding characteristics and quantitation of the recently reported fetal steroid binding protein (FSBP) cannot be determined on unpurified samples; an immunoassay was therefore desirable. The protein was purified to homogeneity in order to raise a highly specific polyclonal antibody. An enzyme-linked immunosorbent ...

journal_title：Steroids

authors： Iqbal MJ,Forbes A,Corbishley TP,Wilkinson ML,Williams R

更新日期：1985-01-01 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：:Based on histological criteria, Kingsley and Bogdanove (3) reported that the benzoate ester of 17beta-hydroxy-5alpha-androstan-3-one (5alpha-DHT), unlike testosterone propionate, is unable to induce vaginal mucification when given subcutaneously to rats. In contrats, Kennedy (4) found in estrogen-pretreated rats that ...

journal_title：Steroids

authors： Kennedy TG,Armstrong DT

更新日期：1976-03-01 00:00:00

abstract：:A series of final twelve propanoyloxy derivatives of 5β-cholan-24-oic acid (O-propanoyl derivatives of cholic acid) as potential drug absorption modifiers (skin penetration enhancers, intestinal absorption promoters) was generated by multistep synthesis. Structure confirmation of all generated compounds was accomplish...

journal_title：Steroids

authors： Coufalová L,Mrózek L,Rárová L,Plaček L,Opatřilová R,Dohnal J,Král'ová K,Paleta O,Král V,Drašar P,Jampílek J

更新日期：2013-05-01 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：: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：:Trimegestone (TMG) is a novel 19-norpregnane progestin under development for hormone replacement therapy and oral contraception. The objective of the current study was to characterize the potency and steroid receptor selectivity of TMG in several in vitro assays and to compare its activity to that of medroxyprogestero...

journal_title：Steroids

authors： Zhang Z,Lundeen SG,Zhu Y,Carver JM,Winneker RC

更新日期：2000-10-01 00:00:00

abstract：:Mouse models of cystic fibrosis (CF) display increased sulfotransferase 1E1 (SULT1E1) activity in hepatocytes of cystic fibrosis transmembrane receptor (CFTR)-deficient animals. SULT1E1 is responsible for the sulfation and inactivation of beta-estradiol (E2) at physiological concentrations. IGF-1 message levels in CFT...

journal_title：Steroids

authors： Li L,He D,Wilborn TW,Falany JL,Falany CN

更新日期：2009-01-01 00:00:00

abstract：:The conjugation reactions of hydration and dehydrogenation catalyzed by the dehydratase and dehydrogenase activities of D-3-hydroxyacyl-CoA dehydratase/D-3-hydroxyacyl-CoA dehydrogenase bifunctional protein (DBP) and enoyl-CoA hydratase/3-hydroxyacyl-CoA dehydrogenase bifunctional protein (LBP) in the side chain degra...

journal_title：Steroids

authors： Kurosawa T,Sato M,Nakano H,Fujiwara M,Murai T,Yoshimura T,Hashimoto T

更新日期：2001-02-01 00:00:00

abstract：:A series of novel 5α, 8α-endoperoxide steroidal hybrid derivatives containing isatin or indole substituents on the C-17 side chain were synthesized and characterized. The preliminary anti-proliferative activity of the compounds against HepG2, MCF-7, HT-29 and HeLa cell lines were investigated. Compounds 7g and 7l disp...

journal_title：Steroids

authors： Li H,Wang H,Wang J,Lin Y,Ma Y,Bu M

更新日期：2020-01-01 00:00:00

abstract：:The syntheses of 15beta-carboxyethylmercapto-5alpha-dihydrotestosterone, 15beta-carbosyethylmercapto-5alpha-androstane-3beta, 17beta-diol and 15beta-carboxyethylmercapto-5alpha-androstane-3alpha, 17beta-diol and the preparation of their bovine serum albumin (BSA) conjugates are described. These conjugates were employe...

journal_title：Steroids

authors： Rao PN,Khan AH,Moore PH Jr

更新日期：1977-02-01 00:00:00