Results 181 to 190 of about 5,290 (236)

Non-Steroidal Subtype Selective Estrogens

Current Medicinal Chemistry, 2005
The biological effects of estrogens are thought to be mediated by two receptors referred to as ERalpha and ERbeta. In recent years significant efforts have been devoted to the design of subtype selective ligands. These ligands are valuable tools to establish the precise biological role of each of the subtypes and to develop new generations of ...
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Identification of a non-steroidal estrogen, equol, in the urine of pregnant macaques: correlation with steroidal estrogen excretion

Journal of Steroid Biochemistry, 1984
Macaque urinary estrogens at late pregnancy were separated by high performance liquid chromatography and quantified, both with radioimmunoassay and an in vitro uterine estrogen receptor assay. Five estrogens were measured. Four were steroids: estriol, estrone, 17 beta-estradiol, and 16 alpha-hydroxyestrone.
S L, Monfort, M A, Thompson, N M, Czekala, L H, Kasman, C H, Shackleton, B L, Lasley   +5 more
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Testicular toxicity and mutagenicity of steroidal and non-steroidal estrogens in the male mouse

Mutation Research/Genetic Toxicology, 1991
The mutagenicity and toxicity of diethylstilbestrol (DES), 17 beta-estradiol and zeranol on the male mouse germ cells were investigated with meiotic micronucleus assays in vivo and in vitro, sperm-head abnormality test and morphometry. Further, the developmental effects of DES on testicular morphology were explored.
L, Pylkkänen, K, Jahnukainen, M, Parvinen, R, Santti   +3 more
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Steroid and non-steroid UDP glucuronyltransferase: Glucuronidation of synthetic estrogens as steroids

Journal of Steroid Biochemistry, 1977
Abstract The hepatic microsomal glucuronidation profiles of eight substrates were investigated; p-nitrophenol (PNP), 4-methylumbelliferone (MUB), 1-naphthol (N), diethylstilbestrol (DES), β-estradiol (E2), estrone (E1), testosterone (T), and phenolphthalein (P).
G W, Lucier, O S, McDaniel
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The synthesis of non-steroidal estrogen receptor binding compounds labeled with 80mBr

International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology, 1986
Estrogen receptor (ER) binding radiopharmaceuticals have potential for use in the diagnosis and treatment of cancers of the female reproductive system. Two triphenylethylene derivatives based on the structure of hydroxytamoxifen 4, a high ER binding metabolite of tamoxifen 5, have been prepared: 1-(4-dimethylaminoethoxy)phenyl]-1-(4-hydroxy)phenyl-2 ...
R H, Seevers, R C, Mease, A M, Friedman, E R, Desombre   +3 more
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The potent and selective inhibition of estrogen production by non-steroidal aromatase inhibitor, YM511

The Journal of Steroid Biochemistry and Molecular Biology, 1995
YM511 inhibited aromatase activities in microsomes from rat ovary and human placenta competitively (IC50s: 0.4 and 0.12 nM, respectively). YM511 was about 3 times more potent than other aromatase inhibitors, such as CGS 16949A, CGS 20267 and R 76713. YM511 decreased the contents of estradiol stimulated by pregnant mare's serum gonadotropin in rat ovary
M, Kudoh, Y, Susaki, Y, Ideyama, T, Nanya, M, Okada, H, Shikama, T, Fujikura   +6 more
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The synthesis of new platinum(II) complexes linked to non-steroidal estrogens

Inorganica Chimica Acta, 1993
Abstract New platinum(II) complexes linked to triphenylethylene are efficiently synthesised in seven steps from desoxyanisoin with an overall yield exceeding 30%. The methodology described gives access to interesting non-steroidal cytotoxic estrogens designed for the treatment of breast cancer.
Penelope Wheeler, Gervais Bérubé
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Hormonal Action of Plant Derived and Anthropogenic Non-Steroidal Estrogenic Compounds: Phytoestrogens and Xenoestrogens

Current Medicinal Chemistry, 2010
Herbivorous and omnivorous vertebrates have evolved in the presence of a variety of phytoestrogens, i.e., plant-derived compounds that can mimic, modulate or disrupt the actions of endogenous estrogens. Since the discovery of the estrus-inducing effects of some plant products in 1926, considerable effort has been devoted to the isolation and structural
T, Lóránd, E, Vigh, J, Garai
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Experimental electron density studies of non-steroidal synthetic estrogens: Diethylstilbestrol and dienestrol

Journal of Molecular Structure, 2008
Abstract An experimental charge density analysis has been carried out on two synthetic estrogens, diethylstilbestrol (DES) and dienestrol (DNS), to further investigate the alignment and binding of estrogenic compounds to the estrogen receptor, and to also establish a relationship between the biological function and the electronic properties of ...
Eric J. Yearley, Elizabeth A. Zhurova, Vladimir V. Zhurov, A. Alan Pinkerton   +3 more
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De novo design, synthesis and evaluation of a non-steroidal diphenylnaphthyl propylene ligand for the estrogen receptor

Bioorganic & Medicinal Chemistry, 2003
There is still a strong need for additional diversity and new chemical scaffolds to allow for the exploration of improved tissue selectivity and finding better selective estrogen receptor modulators (SERMs). Using a de novo design technology a diphenylnaphthyl propylene scaffold, exemplified by (E)-9b, with ER antagonist activity has been generated. It
Jonathan M, Schmidt, Julie, Mercure, Gilles B, Tremblay, Martine, Pagé, Miklos, Feher, Robert, Dunn-Dufault, Markus G, Peter, Peter R, Redden   +7 more
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