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Mario Díaz
European journal of pharmacology, 445(3), 257-266 (2002-06-25)
The nonsteroidal antiestrogens tamoxifen, 4-OH-tamoxifen and toremifene rapidly inhibited spontaneous contractile activity and reduced basal tone in isolated mouse duodenal muscle. Inhibition was rapid in onset ( approximately 2 min) and was not mimicked by the pure steroidal antiestrogen 7alpha-[9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl]-estra-1,3,5(10)-triene-3,17beta-diol...
Xiao-Fang Li et al.
Journal of fluorescence, 21(5), 1969-1977 (2011-05-24)
New aggregation-induced emission (AIE) compounds derived from triphenylethylene were synthesized. The thermal, photophysical, electrochemical and aggregation-induced emissive properties were investigated. All the compounds had strong blue light emission capability and good thermal stability. Their maximum fluorescence emission wavelengths were between...
Ifeyinwa Obiorah et al.
Molecular pharmacology, 85(5), 789-799 (2014-03-13)
Development of acquired antihormone resistance exposes a vulnerability in breast cancer: estrogen-induced apoptosis. Triphenylethylenes (TPEs), which are structurally similar to 4-hydroxytamoxifen (4OHT), were used for mechanistic studies of estrogen-induced apoptosis. These TPEs all stimulate growth in MCF-7 cells, but unlike...
E Mombelli
SAR and QSAR in environmental research, 23(1-2), 37-57 (2011-10-22)
The determination of binding affinities for the estrogen receptor (ER) is used extensively to assess potential hazards to human health and the environment arising from chemicals that can interfere with natural hormone homeostasis. Given the great number of chemicals to...
[The search for active antitumor agents among triphenylethylene derivatives].
P V Sergeev et al.
Voprosy onkologii, 41(2), 49-49 (1995-01-01)
B L Xu et al.
Yao xue xue bao = Acta pharmaceutica Sinica, 36(3), 179-184 (2003-02-13)
In order to improve the biological activity and reduce the side effects and toxicity, a series of novel estrogen receptor antagonists were designed. The key triphenylethylene intermediates were obtained by the McMurry reaction. The target compounds were prepared by etherification....
M Pons et al.
Journal of steroid biochemistry, 36(5), 391-397 (1990-08-14)
The relative binding affinities of a series of twelve para-hydroxylated triphenylethylenes (TPEs) for the estradiol receptor (ER) of calf uterus cytosol were measured by a competition method. The results obtained under equilibrium conditions support the hypothesis of the additivity of...
G Grenier et al.
Chemical & pharmaceutical bulletin, 46(9), 1480-1483 (1998-10-17)
In a previous work we synthesized a class of new antineoplastic drugs by coupling a cisplatin derivative to a triphenylethylene moiety similar to the antiestrogen, tamoxifen. These drugs differ in the number of hydroxy functions on the triphenylethylene rings and...
Effect of estrogenic and antiestrogenic triphenylethylene derivatives on progesterone and estrogen receptors levels of MCF-7 cells.
N Legros et al.
Biochemical pharmacology, 42(9), 1837-1841 (1991-10-09)
MnO 2-promoted carboesterification of alkenes with anhydrides: a facile approach to ?-lactones
Wu Lihuan, et al.
Chemical Communications (Cambridge, England), 52(12), 2628-2631 (2016)
A Séné et al.
Drug design and discovery, 15(4), 277-285 (1999-11-05)
Six new platinum(II) complexes were synthesized from a common triphenylethylene precursor using various diamines. The cytotoxicity of the compounds, evaluated on human breast cancer cell lines (MCF-7 and MDA-MB-231), was greatly influenced by the nature of the diamine ligand. Two...
Chellakkan S Blesson et al.
Steroids, 71(11-12), 993-1000 (2006-09-13)
The study was aimed to investigate the interaction of D,L-ormeloxifene (Orm), a triphenylethylene and its hydroxy derivative with estrogen receptor subtypes alpha and beta, its influence on ERE-driven transcriptional activation and progesterone receptor expression. In competitive binding experiments using human...
S J Gatley et al.
International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology, 18(7), 769-775 (1991-01-01)
A triphenylethylene compound [1,1-bis(4-hydroxyphenyl)-2-iodo-2-phenylethylene; IBHPE] has been labeled by halodestannylation with 123I at a specific radioactivity of 13,200 Ci/mmol (by in vitro receptor assay) after HPLC purification. The corresponding 80mBr-labeled compound (BrBHPE), which has a 3-fold higher affinity for the...
M Diaz et al.
The Journal of physiology, 536(Pt 1), 79-88 (2001-10-02)
1. The regulation of Maxi Cl(-) channels by 17beta-oestradiol and non-steroidal triphenylethylene antioestrogens represents a rapid, non-classical effect of these compounds. In the present study we have investigated the signalling pathways used for the regulation of Maxi Cl(-) channel activity...
E Bignon et al.
FEBS letters, 271(1-2), 54-58 (1990-10-01)
The activation of type I (gamma), II (beta) and III (alpha) protein kinase C (PKC) subspecies by phosphatidylserine (PS) and diacylglycerol (DAG) is inhibited by micromolar concentrations of triphenylacrylonitrile (TPE) antiestrogens. TPE A (with p-hydroxy and p-diethylaminoethoxy groups on the...
E Bignon et al.
Biochemical pharmacology, 42(7), 1373-1383 (1991-09-12)
We have performed a systematic study of the interaction of 36 di- and tri-phenylethylene derivatives (DPEs and TPEs) with protein kinase C (PKC). The results were submitted to a multivariate analysis in order to identify the structural features that might...
T Ojasoo et al.
The Journal of steroid biochemistry and molecular biology, 44(3), 239-250 (1993-03-01)
A multivariate statistical method, correspondence factorial (CF) analysis, was used to examine the correlations among the protein binding and cell proliferation effects of a series of 36 di- and triphenylethylenes (DPEs and TPEs). The analysis was applied to a study...
C D van den Koedijk et al.
Biochemical pharmacology, 46(10), 1870-1872 (1993-11-17)
The binding affinity of derivatives of the triphenylethylene (TPE) antioestrogen tamoxifen and of steroidal compounds for human liver antioestrogen binding sites (AEBS) was compared with their binding affinity for rat liver AEBS. Despite the observation of some quantitative differences overall...
M Metzler et al.
American journal of clinical oncology, 14 Suppl 2, S30-S35 (1991-01-01)
The mechanisms of estrogen-induced cancer are still a matter of debate. Previous studies with stilbene estrogens and steroidal estrogens have shown that the in vitro transformation of primary Syrian hamster embryo (SHE) fibroblasts is a good experimental system for discriminating...
Lifang Zheng et al.
Anti-cancer drugs, 18(9), 1039-1044 (2007-08-21)
Tamoxifen analogs (1-3) and 1,1,2-triphenylethylenes (4-7) have been synthesized by the McMurry coupling reaction. Their antiproliferative effects on MCF-7 human breast-cancer cells, HO-8910 human ovarian-carcinoma cells, and (HL)-60 human promyelocytic-leukemia cells were studied by use of the colorimetric MTT assay...
R V Weatherman et al.
Chemistry & biology, 8(5), 427-436 (2001-05-19)
The selective estrogen receptor modulators (SERMs) raloxifene and tamoxifen are triphenylethylene derivatives that affect transcriptional regulation by the estrogen receptors (ERalpha and ERbeta) but show different effects in different tissues. A third triphenylethylene derivative, GW-5638, displays tissue selectivity in rats...
Speculation on the mechanism of action of triphenylethylene antioestrogens.
C D van den Koedijk et al.
Biochemical pharmacology, 47(11), 1927-1937 (1994-06-01)
E S Lee et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 6(12), 4893-4899 (2001-01-13)
The triphenylethylene antiestrogens, idoxifene (Idox) and toremifene (Tor), are structurally related analogues of tamoxifen (Tam) and were developed to improve the therapeutic index for advanced breast cancer patients. However, the issue of cross-resistance with Tam for these new agents is...
S M Hyder et al.
Cancer letters, 120(2), 165-171 (1998-02-14)
Estradiol induces vascular endothelial growth factor (VEGF) expression in the rat uterus and this may contribute to the hyperemia and increased vascularity produced by estrogens in this target tissue. Triphenylethylene antiestrogens such as tamoxifen have mixed agonist/antagonist activity and their...
Asymmetric epoxidation of alkenes in fluorinated media, catalyzed by second-generation fluorous chiral (Salen) manganese complexes
Cavazzini M, et al.
European Journal of Organic Chemistry, 2001(24), 4639-4649 (2001)
R LE Lain et al.
Journal of enzyme inhibition and medicinal chemistry, 17(2), 93-100 (2002-11-08)
The 7-hydroxycoumarins, umbelliferone and 4-methylumbelliferone (IC50 = 1.4 and 1.9 microM, respectively) were potent inhibitors of human testes microsomal 17beta-HSD (type 3) enzyme whereas 7-methoxycoumarin, 4-hydroxycoumarin and 7-ethoxycoumarin had little or no inhibitory activity. Analogues of the weak inhibitory triphenylethenes...
Yuliya Dobrydneva et al.
Journal of cardiovascular pharmacology, 50(4), 380-390 (2007-12-01)
The anti-estrogenic drug tamoxifen, which is used therapeutically for treatment and prevention of breast cancer, can lead to the development of thrombosis. We found that tamoxifen rapidly increased intracellular free calcium [Ca2+]i in human platelets from both male and female...
H Wiseman et al.
Chemico-biological interactions, 79(2), 229-243 (1991-01-01)
The azole antifungal drug ketoconazole was found to inhibit Fe(III)-ascorbate dependent lipid peroxidation using either rat liver microsomes or ox-brain phospholipid liposomes as the substrate. It also inhibited microsomal peroxidation induced by the Fe(III)-ADP/NADPH system. The related azoles, miconazole and...