Results 101 to 110 of about 12,682 (158)

Organometallic derivatives of estradiol as bioligands: Targetted binding of the estradiol receptor

Journal of Steroid Biochemistry, 1989
The complexation of estrogens by transitional metal units e.g. (alkyne)Co2(CO)6 and (alkyne)Mo2Cp2(CO)4, at the 17 alpha-position brings about a dramatic change in the chemical behavior of these compounds with respect to that of the free ligands. The 17 beta-OH function becomes particularly labile, even in weakly acidic medium, giving rise to carbenium
A, Vessières, C, Vaillant, M, Salmain, G, Jaouen   +3 more
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Synthese und Eigenschaften fluoreszierender Estradiol‐Derivate

Archiv der Pharmazie, 1986
Abstract17β‐Estradiol‐7α‐butansäure (1) wird unter Zusatz von Dicyclohexylcarbodiimid mit Fluoresceinamin zu Estradiol‐7α‐butansäure‐fluoresceinamid (3) gekoppelt. 17β‐Estradiol‐7α‐butylamin (2) reagiert mit Fluorescamin zum entsprechenden Pyrrolinon‐Derivat 4 und mit Fluoresceinisothiocyanat zu Estradiol‐7α‐butyl‐fluoresceinylthiocarbamid (5 ...
Brigitte Mühlenbruch, Friedhelm Kirmeier, Hermann J. Roth   +2 more
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Preparation of B-ring brominated derivatives of estradiol

Steroids, 1986
The preparation of 6 beta-methoxy-7 alpha-bromoestradiol (1) is reported. Addition of in situ-generated BrOMe to 6-dehydroestradiol 3-tetrahydropyranyl ether (4a) afforded the expected addition product. Removal of the tetrahydropyranyl protective group was carried out by mild acid hydrolysis to afford 1 in good yields.
A A, Leon, F A, Mettler, M D, Hylarides
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Synthesis and pharmacological evaluation of 8α-estradiol derivatives

Steroids, 1982
Abstract A number of 2- and 16-alkyl 8α-estradiol derivatives were synthesized and pharmacologically characterized with respect to estrogenic/antiestrogenic activities.
F B, González, G, Neef, U, Eder, R, Wiechert, E, Schillinger, Y, Nishino   +5 more
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Synthesis of new heterocyclic derivatives of estradiol

Tetrahedron, 1971
Abstract The preparation of the steroidal chromone ( 4 ), chromanone ( 5a ), methylbenzoxazole ( 6 ), and methylbenzisoxazole ( 7 ), from the 2-acetyl steroid ( 2a ) and its oxime ( 2d ), is reported. Chromone ( 4 ) is shown to react with hydrazine hydrate and hydroxylamine hydrochloride to provide respectively the 3′-phenylpyrazole ( 10a ) and a ...
P. Crabbé, L.A. Maldonado, I. Sánchez
openaire   +1 more source

Synthesis and receptor binding of polynuclear organometallic estradiol derivatives

Journal of Steroid Biochemistry, 1988
Twelve novel organometallic derivatives of estradiol were synthesized with the aim of utilizing organometallic cold bioprobes as radioisotopic labels substitutes for steroid hormone receptor assays. For this purpose, we envisaged the attachment of several stable cobalt, molybdenum, osmium carbonyl clusters (tetra- and pentanuclear species) at estradiol
A, Vessieres, G, Jaouen, M, Gruselle, J L, Rossignol, M, Savignac, S, Top, S, Greenfield   +6 more
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Estrogen receptor binding tolerance of 16α-substituted estradiol derivatives

Steroids, 1988
In order to examine the tolerance of the estrogen receptor for 16 alpha-substituents in estradiol, we have synthesized various 16 alpha-substituted estrogens and determined their binding affinity for receptor by a competitive radiometric binding assay.
T L, Fevig, M K, Mao, J A, Katzenellenbogen   +2 more
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AN EXPEDITIOUS ROUTE TO 7α-SUBSTITUTED ESTRADIOL DERIVATIVES

Tetrahedron Letters, 1997
Abstract 6-Ketoestradiol derivatives are converted in 7α-alkyl substituted estradiol derivatives selectively by alkylation of the generated enolate followed by deoxygenation-deprotection with BF3·Et2O/Et3SiH. © 1997 Elsevier Science Ltd.
Rosanna Tedesco, John A Katzenellenbogen, Elio Napolitano   +2 more
openaire   +1 more source

Synthesis of 7α-substituted derivatives of 17β-estradiol

Steroids, 2006
Abstract Estrogen receptor (ER) pure antagonists such as ICI-182,780 (fulvestrant) are effective alternatives to tamoxifen (an ER antagonist/weak partial agonist) in the treatment of postmenopausal, receptor-positive human breast cancers. Structurally, these pure antagonists contain the basic core structure of 17β-estradiol (E 2 ) with a long side ...
Xiang-Rong Jiang, J. Walter Sowell, Bao Ting Zhu   +2 more
openaire   +1 more source

17β-Estradiol inhibits keratinocyte-derived chemokine production following trauma-hemorrhage

American Journal of Physiology-Lung Cellular and Molecular Physiology, 2007
Neutrophil infiltration is a key step in the development of organ dysfunction following trauma-hemorrhage (T-H). Although we have previously shown that 17β-estradiol (E2) prevents neutrophil infiltration and organ damage following T-H, the mechanism by which E2 inhibits neutrophil transmigration remains unknown.
Michael, Frink, Bjoern M, Thobe, Ya-Ching, Hsieh, Mashkoor A, Choudhry, Martin G, Schwacha, Kirby I, Bland, Irshad H, Chaudry   +6 more
openaire   +2 more sources