Synthesis and biological evaluation of novel C6-cyclo secondary amine substituted purine steroid-nucleosides analogues.

abstract：:13beta-Ethyl-3-methoxy-17beta-ol-8,14-seco-1,3,5(10),8-gonatetraen-14-one (IIIa) was isolated and its participation in the well-known acidic cyclization process was established. ...

journal_title：Steroids

authors： Makk N,Tóth G,Tömörkény E

更新日期：1975-05-01 00:00:00

abstract：:A series of clickable bile acid-nucleosides conjugates linked directly or via amino acid linker were synthesized, and characterized by spectroscopic techniques such as 1H NMR, 13C NMR, FT-IR, HRMS and HPLC. The synthesized compounds 6a-p were screened for their in vitro anticancer property against a panel of three can...

journal_title：Steroids

authors： Agarwal DS,Siva Krishna V,Sriram D,Yogeeswari P,Sakhuja R

更新日期：2018-11-01 00:00:00

abstract：:The leaky heme mutants G204, G216, and G214 are shown to accumulate exogenous sterols. Unlike hem mutants which have complete blocks in the heme pathway, these strains do not require ergosterol, methionine, or unsaturated fatty acids for growth. The addition of aminolevulinic acid to the growth medium inhibited sterol...

journal_title：Steroids

authors： Shinabarger DL,Keesler GA,Parks LW

更新日期：1989-03-01 00:00:00

abstract：:As demonstrated for pregnenolone, saturated ketones are conveniently alpha-hydroxymethylated by their transformation into a lithium enolate and by the reaction of the latter with formaldehydr. The 17-hydroxymethylpregnenolone prepared by this method in very good yield was readily converted to 17-hydroxymethylprogester...

journal_title：Steroids

authors： Mukherjee D,Engel CR

更新日期：1979-11-01 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：:4- to 8-cell mouse PIE's (preimplantation embryos) were cultured in vitro for 48 hr in media containing various concentrations of the anti-estrogen CI-628. Graded effects of the various concentrations were observed with the highest concentration (1.5 microng/ml) being 100% effective in blocking development to the blas...

journal_title：Steroids

authors： Gupta JS,Dey SK,Dickmann Z

更新日期：1977-03-01 00:00:00

abstract：:In this paper we report the synthesis of four fluorinated analogues of brassinosteroids in which fluorine was introduced stereoselectively at C-2. The bioactivity of these new compounds was evaluated using the rice lamina inclination test. The results show that two of these analogues elicit high bioactivity, suggestin...

journal_title：Steroids

authors： Acebedo SL,Ramírez JA,Galagovsky LR

更新日期：2009-04-01 00:00:00

abstract：:Guinea pig adrenal estrogen sulfotransferase from either sex was eluted as a single peak, irrespective of buffer salt concentration, when subjected to fast protein liquid chromatography on gel filtration columns. The same enzyme was consistently eluted in two distinct peaks during chromatofocusing. Adrenal pregnenolon...

journal_title：Steroids

authors： Glasier MA,Glutek SM,Hobkirk R

更新日期：1992-06-01 00:00:00

abstract：:The properties of 5-ene-3 beta hydroxysteroid oxidoreductase (3 beta-HSD) from human placental homogenates were studied in vitro. The apparent Michaelis constants for 3 beta-HSD with the substrates pregnenolone (delta 5P) and dehydroepiandrosterone (DHA) were 170 nM and nM respectively. The optimal pH for both these s...

journal_title：Steroids

authors： Yoshida N

更新日期：1979-01-01 00:00:00

abstract：:The characterization of new conjugated vitamin D metabolites in rat bile was performed using HPLC, liquid chromatography/tandem mass spectrometry combined derivatization, and GC-MS. After the administration of 24,25-dihydroxyvitamin D(3) to rats, 23, 25-dihydroxy-24-oxovitamin D(3) 23-glucuronide, 3-epi-24, 25-dihydro...

journal_title：Steroids

authors： Higashi T,Miura K,Kikuchi R,Shimada K,Hiyamizu H,Ooi H,Iwabuchi Y,Hatakeyama S,Kubodera N

更新日期：2000-05-01 00:00:00

abstract：:A mechanistic study on the nucleophilic substitution of a strictly geometric 21-bromo-3alpha-hydroxyl-3beta-methoxymethyl-5alpha-pregnan-20-one was described. Reaction of the alpha-bromoketone with excess lithium imidazole followed by the addition of extra bases including n-butyllithium, methyllithium, lithium piperid...

journal_title：Steroids

authors： Chen CY,Wong FF,Lee YH,Chou SY,Huang JJ,Yeh MY

更新日期：2006-11-01 00:00:00

abstract：:A radioimmunoassay (RIA) method is described for the determination of 4-androstene-3, 11, 17-trione (11-oxo-androstenedione) in human plasma. 4-androstene-3, 11, 17-trione 3-(0-carboxymethyl) oxime-bovine serum albumin conjugate was used to generate highly specific antiserum in rabbits. Cross reactivities of several o...

journal_title：Steroids

authors： Schlaghecke R,Kley HK,Krüskemper HL

更新日期：1984-07-01 00:00:00

abstract：:A radioimmunoassay for the quantitation of the sum of free, glucuronidated and urine is described. The method is reliable and accurate. Using this method, urinary excretion of 16 alpha-hydroxyestrone was determined in normal men, premenopausal women, and postmenopausal women. The values were compared to the urinary ex...

journal_title：Steroids

authors： Naganuma H,Hershcopf RJ,Michnovicz JJ,Miyairi S,Bradlow HL,Fishman J

更新日期：1989-01-01 00:00:00

abstract：:Three new pregnane steroids, 2beta,3beta,5beta-trihydroxy-pregn-20-en-6-one (1), 3beta-hydroxy-5alpha-pregn-7,20-dien-6-one (2), and 3beta-acetoxy-5alpha-pregn-7,20-dien-6-one (3) were isolated from the twigs and leaves of Turraea pubescens, and were structurally elucidated on the basis of spectroscopic data and chemi...

journal_title：Steroids

authors： Wang XN,Fan CQ,Yue JM

更新日期：2006-08-01 00:00:00

abstract：:The hydrolysis of 108 esters of norethisterone (17 alpha-ethynyl-17 beta-hydroxyestr-4-en-3-one) was studied in vitro using a rabbit liver preparation. Introduction of a double or triple bond into a straight-chain ester did not inhibit hydrolysis but a marked reduction in hydrolysis was produced on replacement of a me...

journal_title：Steroids

authors： Naderi S,Fotherby K

更新日期：1983-03-01 00:00:00

abstract：:Different phytoestrogens were tested as inhibitors of 17beta-hydroxysteroid dehydrogenase from the fungus Cochliobolus lunatus (17beta-HSDcl), a member of the short-chain dehydrogenase/reductase superfamily. Phytoestrogens inhibited the oxidation of 100microM 17beta-hydroxyestra-4-en-3-one and the reduction of 100micr...

journal_title：Steroids

authors： Kristan K,Krajnc K,Konc J,Gobec S,Stojan J,Lanisnik Rizner T

更新日期：2005-08-01 00:00:00

abstract：:Finasteride is a specific 5 alpha-reductase inhibitor that has been shown to reduce the size of human benign prostatic hyperplasia (BPH) by inhibiting the intraprostatic conversion of testosterone to 5 alpha-dihydrotestosterone. The aim of the present in vitro study was to describe in more detail the inhibitory effect...

journal_title：Steroids

authors： Weisser H,Tunn S,Debus M,Krieg M

更新日期：1994-11-01 00:00:00

abstract：:The potent antiproliferative effect of progestins has been utilized in clinical regimens for treatment of endometrial proliferative disorders. The progestin infiltrated intrauterine device used as therapy for endometrial carcinoma as well as endometrial hyperplasia yields a hundred-fold increase of local progestin con...

journal_title：Steroids

authors： Paulssen RH,Moe B,Grønaas H,Orbo A

更新日期：2008-01-01 00:00:00

abstract：:15alpha-Hydroxydehydroisoandrosterone and 15alpha-hydroxypregnenolone were isolated from hydrolyzed extracts of human late pregnancy urine and identified by means of the isotope dilution technique. In two separate determinations the excretion rate of 15alpha-hydroxydehydroisoandrosterone was found to be 1.7 and 3.2 mi...

journal_title：Steroids

authors： Stanczyk FZ,Stern M,Solomon S

更新日期：1978-05-01 00:00:00

abstract：:Mass spectra and fragmentation patterns of the epimeric 17-, 16-, 15- and 14-hydroxy derivatives of 3-methoxy-1,3,5(10)-estratriene are compared. The main fragmentation pathways are differently influenced, depending on the position of the hydroxy group. The different configuration of the hydroxy groups is reflected on...

journal_title：Steroids

authors： Schade W,Ihn W,Vokoun J,Schönecker B,Schubert G

更新日期：1980-11-01 00:00:00

abstract：:5 alpha-(17R,20R)-14,15-Secocholestane (12) was synthesized from cholesterol (1) in 12 steps. The key intermediate, 5 alpha-cholest-14-en-3 beta-yl acetate (4), underwent ozonization, reduction, hydrolysis, and oxidation to provide 5 alpha-14,15-secocholesta-3,14,15-trione (8). One of the Clemmensen reduction products...

journal_title：Steroids

authors： Li TS,Li YL,Liang XT

更新日期：1990-06-01 00:00:00

abstract：:In humans, the onset of adrenache has been found to occur with the appearance of the zona reticularis, the inner zone of the adrenal cortex. Since an increase in the volume of adrenal cortex during maturation in the guinea pig has been associated with the growth of the zona reticularis, we were interested in investiga...

journal_title：Steroids

authors： Bélanger B,Caron S,Boudou P,Fiet J,Bélanger A

更新日期：1992-02-01 00:00:00

abstract：:A rapid and efficient synthesis of 6E-hydroximinosteroid homodimers is described. The two new compounds were linked at position 3 of the steroid nucleus via a ruthenium catalyzed cross-metathesis reaction. The cytotoxic activity of these compounds was evaluated in vitro on human lung carcinoma A549 (ATCC CCL-185), col...

journal_title：Steroids

authors： Rega M,Jiménez C,Rodríguez J

更新日期：2007-10-01 00:00:00

abstract：:Parathyroid hormone-related protein (PTHrP) increases the growth and osteolytic potential of prostate cancer cells, making it important to control PTHrP expression in these cells. We show that 1,25-dihydroxyvitamin D3 (1,25(OH)2D3) and its non-hypercalcemic analog, EB1089, decrease PTHrP mRNA and cellular protein leve...

journal_title：Steroids

authors： Sepulveda VA,Weigel NL,Falzon M

更新日期：2006-02-01 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：: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：:It has been shown by others that treatment with only progesterone is sufficient to induce implantation and maintain pregnancy in ovariectomized-adrenalectomized rabbits. Based on these results, it was deduced that induction of implantation in the rabbit does not require estrogen. In making this deduction, "blastocyst ...

journal_title：Steroids

authors： Dey SK,Dickmann Z,Sen Gupta J

更新日期：1976-10-01 00:00:00

abstract：:Thyroid hormone receptors (TRs) are nuclear receptors that are activated by thyroid hormone ligands and co-regulator proteins. Two receptor subtypes, TRalpha and TRbeta, have been suggested to play a role in numerous physiological functions. However, specificity of receptor subtype function and co-regulator interactio...

journal_title：Steroids

authors： Koury EJ,Pawlyk AC,Berrodin TJ,Smolenski CL,Nagpal S,Deecher DC

更新日期：2009-02-01 00:00:00

abstract：:While the neuroprotective benefits of estrogen and progesterone in critical illness are well established, the data regarding the effects of androgens are conflicting. Surgical repair of congenital heart disease is associated with significant morbidity and mortality, but there are scant data regarding the postoperative...

journal_title：Steroids

authors： Heckmann M,d'Uscio CH,de Laffolie J,Neuhaeuser C,Bödeker RH,Thul J,Schranz D,Frey BM

更新日期：2014-03-01 00:00:00

abstract：:Testosterone (17 beta -hydroxy-4-androsten-3-one ; T) and dihydrotestosterone (17 beta -hydroxy-5 alpha -androstan-3-one ; DHT) concentrations were determined by radioimmunoassay in different fetal tissues taken from male guinea-pigs. Androgen concentrations were maximal in the components of the Wolffian duct (vas def...

journal_title：Steroids

authors： Rigaudière N

更新日期：1981-08-01 00:00:00