Results 231 to 240 of about 7,787 (278)
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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 +6 more
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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 +6 more
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The synthesis of new platinum(II) complexes linked to non-steroidal estrogens
Inorganica Chimica Acta, 1993Abstract 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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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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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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Current Computer-Aided Drug Design, 2023
Background:Breast cancer is one of the most commonly diagnosed cancer types among women worldwide. Cytochrome P450 aromatase (CYP19A1) is an enzyme in vertebrates that selectively catalyzes the biosynthesis of estrogens from androgenic precursors. Researchers have increasingly focused on developing non-steroidal aromatase inhibitors (NSAIs) for their ...
Khushboo Pandey +5 more
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Background:Breast cancer is one of the most commonly diagnosed cancer types among women worldwide. Cytochrome P450 aromatase (CYP19A1) is an enzyme in vertebrates that selectively catalyzes the biosynthesis of estrogens from androgenic precursors. Researchers have increasingly focused on developing non-steroidal aromatase inhibitors (NSAIs) for their ...
Khushboo Pandey +5 more
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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 +3 more
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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 +3 more
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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 +7 more
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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 +7 more
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Journal of Steroid Biochemistry, 1987
Estrone (E1), estradiol (E2), the catechol estrogens 2-OHE1 and 2-OHE2, and diethylstilbestrol (DES) were incubated with purified prostaglandin synthase (PHS) in vitro in the presence of arachidonic acid and their PHS-catalyzed cooxidation was determined.
G H, Degen +3 more
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Estrone (E1), estradiol (E2), the catechol estrogens 2-OHE1 and 2-OHE2, and diethylstilbestrol (DES) were incubated with purified prostaglandin synthase (PHS) in vitro in the presence of arachidonic acid and their PHS-catalyzed cooxidation was determined.
G H, Degen +3 more
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The Journal of Steroid Biochemistry and Molecular Biology, 1990
CGS 20267 is a new non-steroidal compound which potently inhibits aromatase in vitro (IC50 of 11.5 nM) and in vivo (ED50 of 1-3 micrograms/kg p.o.), CGS 20267 maximally inhibits estradiol production in vitro in LH-stimulated hamster ovarian tissue at 0.1 microM with an IC50 of 0.02 microM and does not significantly affect progesterone production up to ...
A S, Bhatnagar +4 more
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CGS 20267 is a new non-steroidal compound which potently inhibits aromatase in vitro (IC50 of 11.5 nM) and in vivo (ED50 of 1-3 micrograms/kg p.o.), CGS 20267 maximally inhibits estradiol production in vitro in LH-stimulated hamster ovarian tissue at 0.1 microM with an IC50 of 0.02 microM and does not significantly affect progesterone production up to ...
A S, Bhatnagar +4 more
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ChemInform Abstract: The Synthesis of New Platinum(II) Complexes Linked to Non‐Steroidal Estrogens.
ChemInform, 1993AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
P. WHEELER, G. BERUBE
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Bioorganic & Medicinal Chemistry Letters, 1997
Abstract A piperidinoethoxy substituent in non-steroidal antiestrogens has a relatively higher antiestrogenic effects as compared to a pyrrolidinoethoxy moiety. However, the antagonistic activity is more depended on the molecular geometry than the nature of the basic chain.
Sachi Tripathi +4 more
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Abstract A piperidinoethoxy substituent in non-steroidal antiestrogens has a relatively higher antiestrogenic effects as compared to a pyrrolidinoethoxy moiety. However, the antagonistic activity is more depended on the molecular geometry than the nature of the basic chain.
Sachi Tripathi +4 more
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