Abstract:
:Homogeneous catalytic hydrazinocarbonylation of some steroid derivatives possessing iodo-alkenyl moiety (17-iodo-androst-16-ene 1, 17-iodo-3-methoxy-estra-1,3,5(10),16-tetraene 2, 17-iodo-4-aza-4-methyl-androst-16-en-3-one 3 and 17-iodo-6beta-hydroxy-3alpha,5alpha-cycloandrost-16-ene 4) were carried out in the presence of a palladium catalyst, a base and acetic or benzoic hydrazide as the nucleophilic reagent. The corresponding N-acetamido-carbamoyl 1a-4a or N-benzamido-carbamoyl derivatives 1b-4b were obtained in high yields. Some of these derivatives served as starting materials for the synthesis of new steroidal 1,3,4-oxadiazole compounds.
journal_name
Steroidsjournal_title
Steroidsauthors
Szarka Z,Skoda-Földes R,Horváth J,Tuba Z,Kollár Ldoi
10.1016/s0039-128x(02)00006-5subject
Has Abstractpub_date
2002-06-01 00:00:00pages
581-6issue
7eissn
0039-128Xissn
1878-5867pii
S0039128X02000065journal_volume
67pub_type
杂志文章相关文献
STEROIDS文献大全abstract::Saturation analysis of the binding of [3H]dexamethasone [( 3H]DEX) to ammonium sulfate precipitates (ASPs) confirmed the presence of a limited-capacity, high-affinity binder in human adipose tissue cytosols. Various non-radioactive steroids competed with [3H]DEX for binding to the ASPs in the following sequence: dexam...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(87)90091-2
更新日期:1987-06-01 00:00:00
abstract::Glucocorticoids (GCs) and progesterone have been employed as immunosuppressive agents during pregnancy for many years. Intracellular acidification by GCs is due to a rapid non-genomic inhibition of membrane Na(+)/H(+)-exchange 1 (NHE1) activity and is followed by immunosuppression of PHA-stimulated proliferation. NHE1...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2016.01.004
更新日期:2016-07-01 00:00:00
abstract::Steroid delta 4-5 alpha- and delta 4-5 beta-reductase activity was determined in 16 human mammary tumors and 8 DMBA-induced rat mammary tumors using a spectrophotometric assay. Steroid delta 4-5 alpha-reductase was present in all tumors investigated while delta 4-5 beta-reductase was detected in only 6 estrogen recept...
journal_title:Steroids
pub_type: 历史文章,杂志文章
doi:10.1016/s0039-128x(79)80010-0
更新日期:1979-01-01 00:00:00
abstract::Explants prepared from the neocortex and the fetal zone of the human fetal adrenal (gestational age 13 to 18weeks) were maintained under conditions of organ culture for 7 to 9 days during which time they were exposed to hACTH and various related peptides. Corticotrophic activity was monitored by the daily release of d...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(78)90037-5
更新日期:1978-04-01 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
pub_type: 杂志文章
doi:10.1016/j.steroids.2015.01.005
更新日期:2015-07-01 00:00:00
abstract::A cytochrome P450-deficient mutant of the pathogenic fungus, Candida albicans, which accumulates exclusively 14 alpha-methylsterols in place of the normal end product sterol, ergosterol, was examined for alterations in membrane fluidity by electron paramagnetic resonance. The results using four nitroxyl spin labels in...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(89)90032-9
更新日期:1989-03-01 00:00:00
abstract::Cortisol 21-amine (21-amino-11beta,17-dihydroxy-4-pregnene-3,20-dione) was prepared and an enzyme immunoassay for cortisol in serum was established using cortisol 21-amine conjugated with alkaline phosphatase. The minimal amount of cortisol detected was 1ng/tube and the measurable range was from 1 to 80 microgram/d1, ...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(78)90106-x
更新日期:1978-07-01 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
pub_type: 杂志文章
doi:10.1016/0039-128x(92)90004-s
更新日期:1992-04-01 00:00:00
abstract::Biotransformation of a synthetic progestonic hormone dydrogesterone (1), C21H28O2, with a plant pathogenic fungus Macrophomina phaseolina yielded two new 2 and 3, and a known 4 metabolites. These analogues were identified as, 3β,11α-dihydroxy-5β,9β,10α-pregna-7-ene-6,20-dione (2), 15β-hydroxy-9β,10α-pregna-4,6-diene-3...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2018.12.009
更新日期:2019-03-01 00:00:00
abstract::2,2,6,6-Tetramethyl piperidine-N-oxyl nitroxyls are known to partition between aqueous and lipid phases, thus serving as probes to study membrane dynamics. The synthesis of a novel steroidal spin label, 3alpha-hydroxycholan-24-yl-(2",2",6",6"-tetramethyl-N-oxyl)p iperidyl butan-1',4'-dioate, containing 2,2,6,6-tetrame...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(99)00072-0
更新日期:1999-12-01 00:00:00
abstract::Two new sterols, (24E)-24-n-propylidenecholesterol and 24 epsilon-n-propylcholesterol, were isolated from a cultured marine Chrysophyte. Since most of the steroids found in marine invertebrates are unchanged or modified sterols of algal or symbiotic origin, the discovery of these two unusual sterols in a unicellular a...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(80)90104-x
更新日期:1980-02-01 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
pub_type: 杂志文章
doi:10.1016/s0039-128x(00)00217-8
更新日期:2001-02-01 00:00:00
abstract::Dehydroepiandrosterone (DHEA) is an endogenous steroid hormone involved in a number of biological actions in humans and rodents, but its effects on renal tissue have not yet been fully understood. The aim of this study is to assess the effect of DHEA treatment on diabetic rats, mainly in relation to renal function and...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2011.02.006
更新日期:2011-05-01 00:00:00
abstract::The LNCaP-Fast Growing Colony (FGC) human prostate cancer cell line proliferates in response to the addition of dihydrotestosterone (DHT) 10(-10)-10(-8) M in charcoal-stripped serum-supplemented media. LNCaP-FGC cells will not attach or proliferate in serum-free conditions. LNCaP-FGC stock cultures were maintained in ...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(93)90084-z
更新日期:1993-09-01 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
pub_type: 杂志文章
doi:10.1016/s0039-128x(01)00098-8
更新日期:2001-09-01 00:00:00
abstract::The effect of a substituent in the 12-position of progestagens was studied. To this end, various approaches toward the preparation of 12 beta-alkyl- and 12-alkylidenenorpregnanes were investigated. Eventually, the desired compounds 17 beta-hydroxy-12 beta-methyl-18a-homo-19-nor-17 alpha-pregn-4-en-20-yn-3-one (37) and...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(92)90020-a
更新日期:1992-11-01 00:00:00
abstract::Brassinosteroids (BRs) control several important agronomic traits, such as strengthening resistance to diverse adversity, improving the quality, and increasing crop yield. Their chemical structures and varieties, specific methods for the evaluation of bioactivities, structure-activity relationships, potential novel co...
journal_title:Steroids
pub_type: 杂志文章,评审
doi:10.1016/j.steroids.2017.05.005
更新日期:2017-08-01 00:00:00
abstract::To gain further insight into the mechanism for inactivation of aromatase by androst-5-ene-7,17-dione (1) and its 19-nor analog 4, 10 beta-oxygenated steroids 5 and 6, delta 1(10)-steroid 7, and 19-oxo-5 beta,6 beta-epoxy compound 8 were synthesized and tested for their ability to inhibit aromatase in human placental m...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(97)00002-0
更新日期:1997-07-01 00:00:00
abstract::The efficiencies for estrogen conjugate hydrolysis were compared between enzyme hydrolysis, acid solvolysis and a new method, ammonolysis. Samples included: 1) crystalline 1,3,5(10)-estratriene-3, 17 beta-diol disulfate (estradiol 3,17-disulfate), 2) squirrel monkey urine collected following an intravenous injection o...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(84)90023-0
更新日期:1984-06-01 00:00:00
abstract::Sedentary lifestyle and over-nutrition are the main causes of obesity and type 2 diabetes (T2D). However, the same causes are major triggers of hypogonadism. Many T2D patients show low testosterone levels while hypogonadal men seem to be prone to become diabetic. Testosterone plays a major role in the regulation of mu...
journal_title:Steroids
pub_type: 杂志文章,评审
doi:10.1016/j.steroids.2018.08.002
更新日期:2018-10-01 00:00:00
abstract::The synthesis of delta 7,9(11)-lanostadiene derivatives functionalized at C(32) starting from 3 beta-acetoxy-7 alpha,32-epoxylanostan-11-one has been presented. The delta 7,9(11) moiety was efficiently introduced in three steps in 71% yield by the regioselective abstraction of allylic 8 beta hydrogen. The formyl group...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(97)00075-5
更新日期:1997-11-01 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
pub_type: 杂志文章
doi:10.1016/j.steroids.2013.07.006
更新日期:2013-12-11 00:00:00
abstract::Efforts to develop a novel class of nonsteroidal aromatase inhibitors began with the discovery that the infertility in male rats exposed to high levels of the agricultural fungicide, fenarimol (alpha-(2-chlorophenyl)-alpha-(4-chlorophenyl)-5-pyrimidine-methanol), was attributable to the inhibition of aromatase activit...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(83)90072-7
更新日期:1987-07-01 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
pub_type: 杂志文章
doi:10.1016/0039-128x(83)90068-5
更新日期:1987-07-01 00:00:00
abstract::Recent studies by several research groups have shown that G protein estrogen receptor-1 (GPER) formerly known as GPR30, mediates 17beta-estradiol (E2) activation of signal transduction pathways in a variety of human cancer cells and displays E2 binding typical of a membrane estrogen receptor. However, the importance o...
journal_title:Steroids
pub_type: 杂志文章,评审
doi:10.1016/j.steroids.2009.11.005
更新日期:2010-08-01 00:00:00
abstract:OBJECTIVE:Abnormal secretion of thyroid hormones, growth hormone, cortisol and androgens influences body composition. We hypothesised that higher cortisol excretion, in combination with higher androgen and IGF-I concentrations, had a synergistic, favourable effect on body mass and bone. DESIGN, PATIENTS AND METHODS:Th...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2016.09.006
更新日期:2016-11-01 00:00:00
abstract::In this study, we investigated the binding characteristics of [3H]Delta(5)-androstene-3beta,17beta-diol to rabbit vaginal cytosolic and nuclear extracts and in freshly excised intact tissue strips. [3H]delta(5)-Androstene-3beta,17beta-diol bound to a protein(s) in the vaginal nuclear extract with high affinity (K(d)=3...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2003.10.006
更新日期:2004-01-01 00:00:00
abstract::Steroid research at Lederle was initiated in 1946 and continued until about 1971. The areas of research interest involved primarily a study of delta 5,7-steroids, provitamin D3 variants, dehydroepiandrosterone variants, steroidal ketals, corticoids, and steroid conjugates. One of the principal goals was to develop nov...
journal_title:Steroids
pub_type: 历史文章,杂志文章
doi:10.1016/0039-128x(92)90083-l
更新日期:1992-08-01 00:00:00
abstract:BACKGROUND:Once a septic condition is progressing, administration of steroids in the pro-inflammatory phase of septic shock ought to yield maximal effect on the subsequent, devastating inflammatory response. Recently, a retrospective study showed that early initiation of corticosteroid therapy improved survival in sept...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2012.06.001
更新日期:2012-09-01 00:00:00
abstract::Oxidative stress is thought to play a crucial role in the pathogenesis of chronic diabetic complications. We investigated the protective effects of 17 beta-estradiol (E2) on alloxan-induced stress oxidant, hepatic dysfunction and histological changes in male rats liver and pancreas. Our results showed that 17 beta-est...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2007.12.026
更新日期:2008-05-01 00:00:00