35086-46-5Relevant academic research and scientific papers
Synthesis of Triphenylethylene Bisphenols as Aromatase Inhibitors That Also Modulate Estrogen Receptors
Lv, Wei,Liu, Jinzhong,Skaar, Todd C.,O'Neill, Elizaveta,Yu, Ge,Flockhart, David A.,Cushman, Mark
, p. 157 - 170 (2016)
A series of triphenylethylene bisphenol analogues of the selective estrogen receptor modulator (SERM) tamoxifen were synthesized and evaluated for their abilities to inhibit aromatase, bind to estrogen receptor α (ER-α) and estrogen receptor β (ER-β), and antagonize the activity of β-estradiol in MCF-7 human breast cancer cells. The long-range goal has been to create dual aromatase inhibitor (AI)/selective estrogen receptor modulators (SERMs). The hypothesis is that in normal tissue the estrogenic SERM activity of a dual AI/SERM could attenuate the undesired effects stemming from global estrogen depletion caused by the AI activity of a dual AI/SERM, while in breast cancer tissue the antiestrogenic SERM activity of a dual AI/SERM could act synergistically with AI activity to enhance the antiproliferative effect. The potent aromatase inhibitory activities and high ER-α and ER-β binding affinities of several of the resulting analogues, together with the facts that they antagonize β-estradiol in a functional assay in MCF-7 human breast cancer cells and they have no E/Z isomers, support their further development in order to obtain dual AI/SERM agents for breast cancer treatment.
TRIPHENYLETHYLENE COMPOUNDS AND USES THEREOF
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Paragraph 0140, (2017/06/19)
Triphenylethylene compounds as dual aromatase inhibitors and selective estrogen receptors modulators are described. Also described are methods for treating patients of breast cancers, and patients of breast cancer comorbid with osteoporosis, using the des
Iridium-catalyzed arene ortho -silylation by formal hydroxyl-directed C-H activation
Simmons, Eric M.,Hartwig, John F.
supporting information; experimental part, p. 17092 - 17095 (2011/03/01)
A strategy for the ortho-silylation of aryl ketone, benzaldehyde, and benzyl alcohol derivatives has been developed in which a hydroxyl group formally serves as the directing element for Ir-catalyzed arene C-H bond activation. One-pot generation of a (hyd
2-Amino-4-[3′-hydroxyphenyl]-4-hydroxybutanoic acid; A potent inhibitor of rat and recombinant human kynureninase
Walsh, Harold A.,Leslie, Pauline L.,O'Shea, Karen C.,Botting, Nigel P.
, p. 361 - 363 (2007/10/03)
A novel structural analogue of kynurenine, 2-amino-4-[3′-hydroxyphenyl]-4-hydroxybutanoic acid 6, was synthesised as an inhibitor of kynureninase. The compound had a significant inhibitory effect on kynureninase from both rat and human, giving a Ki/
