An efficient one-pot synthesis generating 4-ene-3,6-dione functionalised steroids from steroidal 5-en-3beta-ols using a modified Jones oxidation methodology.

abstract：:17-Hydroxyprogesterone is a well-known precursor of androstenedione in adrenal biosynthesis. This study using sheep adrenal incubations demonstrates that 11-deoxycortisol, the precursor of cortisol synthesis, also can be a precursor of androstenedione. Indeed, our data show that androstenedione synthesis is negatively...

journal_title：Steroids

authors： Auzéby A,Bogdan A,Touitou Y

更新日期：1991-01-01 00:00:00

abstract：:Sertoli cells isolated from 17 day old rats were maintained in culture and incubated with [14C]-progesterone for 20 h. The cells and media were extracted with ether/chloroform and the extracts chromatographed two-dimensionally on TLC and the radioactive metabolites visualized by autoradiography. Nine of the metabolite...

journal_title：Steroids

authors： Wiebe JP,Tilbe KS,Buckingham KD

更新日期：1980-05-01 00:00:00

abstract：:Studies were carried out on the effect of oxygen tension on progesterone (P) accumulation in rat granulosa cell cultures. At 1-2% oxygen, basal, luteinizing hormone (LH)-stimulated, and follicle stimulating hormone (FSH)-stimulated P accumulations were 20, 18, and 11%, respectively, of P levels at 20% oxygen. Basal P ...

journal_title：Steroids

authors： Koos RD,Feiertag MA

更新日期：1989-11-01 00:00:00

abstract：:A series of novel methyl spongoate (1) analogs has been synthesized and evaluated for their in vitro cytotoxic properties. It was found that the nature of the C-20 side chain had significant effects on their bioactivities and some analogs showed higher cytotoxicity than 1 against A549, HCT-116, HepG2, SW-1990, MCF-7 a...

journal_title：Steroids

authors： Jiang CS,Huang CG,Feng B,Li J,Gong JX,Kurtán T,Guo YW

更新日期：2010-12-12 00:00:00

abstract：:The in vivo retention of 3-H-testosterone, dihydrotestosterone (DHT), 3alpha-androstanediol (3alpha-DIOL), 3beta-DIOL, androstenedione, progesterone and cortisol by renal cytoplasm and nuclei of male and female mice was studied. Testosterone was the major androgen isolated from cytoplasm and nuclei following testoster...

journal_title：Steroids

authors： Bullock LP,Bardin CW

更新日期：1975-01-01 00:00:00

abstract：:The effects of progesterone, its agonists (progestin RU-5020, glucocorticoid RU-26988) and antagonist (antiprogesterone, anti-glucocorticoid RU-486) were tested on isolated fat cells in vitro. When added to the incubation medium, all four steroids decreased basal glucose oxidation. The inhibitory effect of the steroid...

journal_title：Steroids

authors： Sutter-Dub MT,Kaaya A,Sfaxi Al,Sodoyez-Goffaux F,Sodoyez JC,Sutter BC

更新日期：1988-11-01 00:00:00

abstract：:The preparation of 9alpha, 11xi-tritiated 17alpha-ethinyl estradiol, mestranol, estradiol-17beta, and norethindrone are described. Estrone-3-methyl ether was employed as starting material, and ethinylation with lithium acetylide-ethylene diamine resulted in 95% mestranol. Demethylation of mestranol with boron tribro...

journal_title：Steroids

authors： Rao PN

更新日期：1971-08-01 00:00:00

abstract：:Recent studies have suggested that progestins play a role in the etiology of breast cancer; however, the mechanisms by which progestins promote tumor formation/progression have not been defined. Progestin action, in target tissues such as the breast, is mediated by the progesterone receptor (PR). PR signaling is compl...

journal_title：Steroids

authors： Treviño LS,Bingman WE 3rd,Edwards DP,Nl W

更新日期：2013-06-01 00:00:00

abstract：:In an attempt to synthesize compounds with selective estrogen-receptor binding, fluoro- and amino-clomiphene were totally synthesized from benzyl chloride, and their estrogenic/antiestrogenic activity as well as that of some of their chemical intermediates was evaluated. The triazene prepared from the amino-clomiphene...

journal_title：Steroids

authors： Gazit A,Livshitz T,Shani J

更新日期：1986-07-01 00:00:00

abstract：:The synthesis of the esters of norethisterone (17 alpha-ethynyl-17 beta-hydroxyestr-4-en-3-one) with three bile acids and of the cholesteryl carbonate of norethisterone are described. :This article reports the synthesis of the esters of norethisterone (17 alpha-ethynl-17beta-hydroxyestr-4-en-3-one) with 3 bile acids ...

journal_title：Steroids

authors： Herz JE,Sandoval J

更新日期：1983-03-01 00:00:00

abstract：:An efficient procedure for the chemical synthesis of 3 beta-hydroxy-5 alpha-cholest-8-en-7-one and 3 beta-hydroxy-5 alpha-cholest-8-en-11-one is described. These ketosterols have been shown to have possible significant hypocholesterolemic effects when fed to normal rats at a level of 0.15% in a laboratory chow diet. T...

journal_title：Steroids

authors： Parish EJ,Nanduri VB,Seikel JM,Kohl HH,Nusbaum KE

更新日期：1986-11-01 00:00:00

abstract：:11 beta-hydroxysteroid dehydrogenase (11 beta-HSD), by converting cortisol and corticosterone to hormonally inactive cortisone and 11-dehydrocorticosterone, respectively, is an important pre-receptor signaling pathway for the renal mineralocorticoid receptor (MR). This receptor has an equal affinity for the glucocorti...

journal_title：Steroids

authors： Stewart PM,Mason JI

更新日期：1995-01-01 00:00:00

abstract：:During our studies of the hepatic androgen receptor in cynomolgus monkeys, tritiated mibolerone +/- a 200-fold excess of unlabeled mibolerone has been used to determine specific binding in cytosol. During time-course studies, high-capacity, unsaturable binding of [3H]mibolerone was noted after short-term incubations (...

journal_title：Steroids

authors： Koritnik DR,Marschke KB,Koshy A

更新日期：1995-11-01 00:00:00

abstract：:An enzyme immunoassay for estrone in swine serum was established. For this, beta-galactosidase from E. coli was conjugated through estrone-17 (O-carboxymethyl)oxime using a mixed anhydride reaction. The percentage of immunoreactive estrone-17 (O-carboxymethyl)oxime-beta-galactosidase conjugate was estimated to be abou...

journal_title：Steroids

authors： Tamamura F,Nakao T,Tsunoda N,Kawata K

更新日期：1982-06-01 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：:Using cultured Y-1 mouse adrenal tumor cells which produce 20 alpha-hydroxy-4-pregnen-3-one (20-DHP), it was found that 0.01 mM corticosterone and deoxycorticosterone increased basal and inhibited ACTH-induced 20-DHP production during consecutive 30 and 120 min incubations. Steroid effects were concentration-dependent...

journal_title：Steroids

authors： Mattson MP,Mrotek JJ

更新日期：1985-07-01 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：:Rat uterine luminal epithelial cells (LEC) responded differently when exposed to an injection of 1.0 microgram estradiol-17 beta (E2) compared to a continuous infusion of E2 at the rate of 1.0 microgram/24 hours. After injection or beginning infusion, LEC mean nuclear area significantly decreased by 4 h, then increase...

journal_title：Steroids

authors： Lavia LA,Roberts DK,Walker NJ,Anderson K

更新日期：1985-06-01 00:00:00

abstract：:In comparison with the glucocorticoids cortisol and corticosterone, the mineralocorticoid aldosterone is a minority hormone of the mammalian adrenal cortex, and its proper function is dependent upon protective physiological mechanisms. These include a particular site of aldosterone synthesis in zona glomerulosa cells ...

journal_title：Steroids

authors： Müller J

更新日期：1995-01-01 00:00:00

abstract：:We report the synthesis of 10 novel steroids obtained from 3 beta, 15 beta-diacetoxy-17 alpha-hydroxy-5-pregnen-20-one (1c) as intermediates in the synthesis of 15 beta-acetoxy-20,20-ethylenedioxy-17 alpha-hydroxy-4-pregnen-3-one (6a) and its tritiated tracer 15 beta-acetoxy-20,20-ethylenedioxy-17 alpha-hydroxy-1,2,6,...

journal_title：Steroids

authors： Reeder AY,Joannou GE

更新日期：1997-02-01 00:00:00

abstract：:The uterine milk (UTM) proteins are the major progesterone-regulated proteins secreted by the sheep uterus during pregnancy. Recently, proteins related to the UTM proteins have been identified in uterine secretions of the pregnant cow and sow. The present objective was to determine the time course for induction of the...

journal_title：Steroids

authors： Leslie MV,Hansen PJ

更新日期：1991-12-01 00:00:00

abstract：:In the present study, synthesis and antineoplastic activity of phenylacetic acid and benzoic acid nitrogen mustard conjugates of various steroidal oximes are reported for the first time. The conjugation was achieved through a more stable oxime-ester linkage and the resulting newly synthesized conjugates were evaluated...

journal_title：Steroids

authors： Acharya PC,Bansal R

更新日期：2017-07-01 00:00:00

abstract：:A series of amphiphilic derivatives of (3β,17β)-3-hydroxyandrost-5-ene-17-carboxylic acid (1) with the polyamine spermine and three other diamines, 1,2-diaminoethane, piperazine and cadaverine, were synthesized and their antimicrobial activity and cytotoxicity were investigated. Among the target compounds, several one...

journal_title：Steroids

authors： Özdemir Z,Bildziukevich U,Šaman D,Havlíček L,Rárová L,Navrátilová L,Wimmer Z

更新日期：2017-12-01 00:00:00

abstract：:CGS 16949A inhibited the conversion of [4-14C]androstenedione (A) to [4-14C]estrone by human placental microsomes in a competitive manner (Ki = 1.6 nM). Aminoglutethimide, also a competitive inhibitor, had a Ki = 0.7 microM in this assay system. The Km for the aromatization of A was 0.11 microM. Using ovarian microsom...

journal_title：Steroids

authors： Steele RE,Mellor LB,Sawyer WK,Wasvary JM,Browne LJ

更新日期：1987-07-01 00:00:00

abstract：:Starting from the structure of ice (in which each water molecule is surrounded by other four water molecules forming a tetrahedron with a value of 4.51Å for the edge O-O distance), and the knowledge that this value also corresponds to the O7-O12 distance of the skeleton of cholic acid, it is hypothesized that two ster...

journal_title：Steroids

authors： Soto VH,Alvarez M,Meijide F,Trillo JV,Antelo A,Jover A,Galantini L,Tato JV

更新日期：2012-10-01 00:00:00

abstract：:The accurate analysis of trace components in complex biological matrices requires the use of reliable internal standards. For liquid chromatography/mass spectrometry analysis, the stable isotope-labeled analogues of the analyte molecules are the most appropriate internal standards. In this paper the synthesis of the 3...

journal_title：Steroids

authors： Mitamura K,Mabuchi T,Nagae K,Nakajima M,Matsumoto R,Fujioka S,Sato K,Satoh née Okihara R,Iida T,Ogawa S,Hofmann AF,Ikegawa S

更新日期：2012-11-01 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 addition of molybdate to rabbit liver cytosol increased significantly the affinity of the glucocorticoid receptor for [3H] dexamethasone without influencing the concentration of binding sites. This effect was concentration dependent. Analysis of the binding data by curve-fitting and Scatchard plot revealed the occ...

journal_title：Steroids

authors： Blanchardie P,Lustenberger P,Orsonneau JL,Denis M,Bernard S

更新日期：1984-08-01 00:00:00

abstract：:Spinasterol and schottenol, two phytosterols present in argan oil and in cactus pear seed oil, were synthesized from commercially available stigmasterol by a four steps reactions. In addition, the effects of these phytosterols on cell growth and mitochondrial activity were evaluated on 158N murine oligodendrocytes, C6...

journal_title：Steroids

authors： Badreddine A,Karym el M,Zarrouk A,Nury T,El Kharrassi Y,Nasser B,Cherkaoui Malki M,Lizard G,Samadi M

更新日期：2015-07-01 00:00:00

abstract：:Two isoforms of the androgen receptor (AR-A and AR-B), differing by a lack of the first 187 amino acids in the NH2-terminal transactivation domain of AR-A, are expressed in connective tissue and bone. Transient transfections of normal human osteoblastic cells (HOB) and of genital skin fibroblasts defective in AR (GSF-...

journal_title：Steroids

authors： Liegibel UM,Sommer U,Boercsoek I,Hilscher U,Bierhaus A,Schweikert HU,Nawroth P,Kasperk C

更新日期：2003-12-01 00:00:00