-
1
-
-
0037435046
-
Antiestrogens and selective estrogen receptor modulators as multifunctional medicines., receptor interactions
-
For recent reviews, see the following: (a) Jordan, V. C. Antiestrogens and Selective Estrogen Receptor Modulators as Multifunctional Medicines., Receptor Interactions. J. Med. Chem. 2003, 46, 883-908.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 883-908
-
-
Jordan, V.C.1
-
2
-
-
0037468902
-
Antiestrogens and selective estrogen receptor modulators as multifunctional medicines, clinical considerations and new agents
-
(b) Jordan, V. C. Antiestrogens and Selective Estrogen Receptor Modulators as Multifunctional Medicines, Clinical Considerations and New Agents. J. Med. Chem. 2003, 46, 1081-1111.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 1081-1111
-
-
Jordan, V.C.1
-
3
-
-
0037434618
-
Selective estrogen-receptor modulators-mechanisms of action and application to clinical practice
-
(c) Riggs, B. L.; Hartmann, L. C. Selective Estrogen-Receptor Modulators-Mechanisms of Action and Application to Clinical Practice. N. Engl. J. Med. 2003, 348, 618-629.
-
(2003)
N. Engl. J. Med.
, vol.348
, pp. 618-629
-
-
Riggs, B.L.1
Hartmann, L.C.2
-
4
-
-
0034954706
-
Physiology of hot flashes
-
(d) Freedman, R. R. Physiology of Hot Flashes. Am. J. Hum. Biol. 2001, 13, 454-464.
-
(2001)
Am. J. Hum. Biol.
, vol.13
, pp. 454-464
-
-
Freedman, R.R.1
-
5
-
-
0036843764
-
Pathphysiology and treatment of hot flashes
-
(a) Shanafelt, T. D.; Barton, D. L.; Adjei, A. A.; Loprinzi, C. L. Pathphysiology and Treatment of Hot Flashes. Mayo Clin. Proc. 2002, 77, 1207-1218.
-
(2002)
Mayo Clin. Proc.
, vol.77
, pp. 1207-1218
-
-
Shanafelt, T.D.1
Barton, D.L.2
Adjei, A.A.3
Loprinzi, C.L.4
-
6
-
-
0038504527
-
Local estrogen treatment in patients with urogenital symptoms
-
For recent reports, see the following: Simunic, V.; Banovic, I.; Ciglar, S.; Jeren, L.; Pavicic Baldani, D.; Sprem, M. Local estrogen treatment in patients with urogenital symptoms. Intl. J. Gynecol. Obstet. 2003, 82 (2), 187-197
-
(2003)
Intl. J. Gynecol. Obstet.
, vol.82
, Issue.2
, pp. 187-197
-
-
Simunic, V.1
Banovic, I.2
Ciglar, S.3
Jeren, L.4
Pavicic Baldani, D.5
Sprem, M.6
-
7
-
-
0036373440
-
SERMs: Evolutionary chemistry, revolutionary biology
-
(b) Miller, C. P. SERMs: Evolutionary Chemistry, Revolutionary Biology. Curr. Pharm. Des. 2002, 8 (23), 2089-2111
-
(2002)
Curr. Pharm. Des.
, vol.8
, Issue.23
, pp. 2089-2111
-
-
Miller, C.P.1
-
8
-
-
18844458270
-
SERMs: Evolutionary chemistry, revolutionary biology
-
(c) Kenemans, P.; Speroff, L. SERMs: Evolutionary Chemistry, Revolutionary Biology. Maturitas 2005, 51 (1), 21-28
-
(2005)
Maturitas
, vol.51
, Issue.1
, pp. 21-28
-
-
Kenemans, P.1
Speroff, L.2
-
9
-
-
13144295008
-
Acta obstetrician a study on urogenital complaints of postmenopausal women aged 50 and over
-
(d) Oskay, U. Y.; Beji, N. K.; Yalcin, O. Acta obstetrician A study on urogenital complaints of postmenopausal women aged 50 and over. Gynecol. Scand. 2005, 84 (1), 72-78.
-
(2005)
Gynecol. Scand.
, vol.84
, Issue.1
, pp. 72-78
-
-
Oskay, U.Y.1
Beji, N.K.2
Yalcin, O.3
-
10
-
-
0029586198
-
Urogenital aging: An old problem newly recognized
-
(e) Bachmann G. Urogenital aging: an old problem newly recognized. Maturitas 1995, 22 Suppl S1-S5.
-
(1995)
Maturitas
, vol.22
, Issue.SUPPL.
-
-
Bachmann, G.1
-
12
-
-
0033649898
-
Selective estrogen receptor modulators (SERMs) in clinical practice
-
(b) Plouffe, L., Jr.; Facoq, C. M. Selective Estrogen Receptor Modulators (SERMs) in Clinical Practice. J. Soc. Gynecol. Invest. 2000, 7, S38-S46.
-
(2000)
J. Soc. Gynecol. Invest.
, vol.7
-
-
Plouffe Jr., L.1
Facoq, C.M.2
-
13
-
-
0032547326
-
Randomized trial of estrogen plus progestin for secondary prevention of coronary heart disease in postmenopausal women
-
(a) Hulley, S.; Grady, D.; Bush, T.; et al. Randomized Trial of Estrogen plus Progestin for Secondary Prevention of Coronary Heart Disease in Postmenopausal Women. J. Am. Med. Assoc. 1998, 280, 605-613.
-
(1998)
J. Am. Med. Assoc.
, vol.280
, pp. 605-613
-
-
Hulley, S.1
Grady, D.2
Bush, T.3
-
14
-
-
0030843969
-
Breast cancer and hormone replacement therapy
-
(b) Collaborative Group on Hormonal Factors in Breast Cancer. Breast Cancer and Hormone Replacement Therapy. Lancet 1997, 350, 1047-1059
-
(1997)
Lancet
, vol.350
, pp. 1047-1059
-
-
-
15
-
-
20844460955
-
Synthesis and structure-activity relationships of analogues of EM-652 (acolbifene), a pure selective estrogen receptor modulator
-
(c) Gauthier, Sylvain; Cloutier, Julie; Dory, Yves L.; Favre. Alexandre; Mailhot, Josee; Quellet, Carl; Schwerdtfeger. Annette: Merand, Yves; Martel, Celine; Simard, Jacques; Labrie, Fernand. Synthesis and structure-activity relationships of analogues of EM-652 (acolbifene), a pure selective estrogen receptor modulator. J. Enzyme Inhib. Med. Chem. 2005, 20 (2), 165-177.
-
(2005)
J. Enzyme Inhib. Med. Chem.
, vol.20
, Issue.2
, pp. 165-177
-
-
Gauthier, S.1
Cloutier, J.2
Dory Yves, L.3
Alexandre, F.4
Mailhot, J.5
Quellet, C.6
Annette, S.7
Merand, Y.8
Martel, C.9
Simard, J.10
Labrie, F.11
-
16
-
-
15144355781
-
Synthesis and pharmacology of conformationally restricted raloxifene analogues: Highly potent selective estrogen receptor modulators
-
(d) Grese, T. A.; Pennington, L. D.; Sluka, J. P.; Adrian, M. D.; Cole, H. W.; Fuson, T. R.; Magee, D. E.; Phillips, D. L.; Rowley, E. R.; Shetler, P. K.; Short, L. L.; Venugopalan, M.; Yang, N. N.; Sato, M.; Glasebrook, A. L.; Bryant, H. U. Synthesis and pharmacology of conformationally restricted raloxifene analogues: highly potent selective estrogen receptor modulators. J. Med. Chem. 1998, 41, 1272.
-
(1998)
J. Med. Chem.
, vol.41
, pp. 1272
-
-
Grese, T.A.1
Pennington, L.D.2
Sluka, J.P.3
Adrian, M.D.4
Cole, H.W.5
Fuson, T.R.6
Magee, D.E.7
Phillips, D.L.8
Rowley, E.R.9
Shetler, P.K.10
Short, L.L.11
Venugopalan, M.12
Yang, N.N.13
Sato, M.14
Glasebrook, A.L.15
Bryant, H.U.16
-
17
-
-
0033013227
-
Adverse events reported by postmenopausal women in controlled trials with raloxifene
-
(a) Davies, G. C.; Huster, M. W. J.; Lu, Y.; Plouffe, L., Jr.; Lakshmanan, M. Adverse Events Reported by Postmenopausal Women in Controlled Trials with Raloxifene. Obstet. Gynecol. 1999, 93, 558-565.
-
(1999)
Obstet. Gynecol.
, vol.93
, pp. 558-565
-
-
Davies, G.C.1
Huster, M.W.J.2
Lu, Y.3
Plouffe Jr., L.4
Lakshmanan, M.5
-
18
-
-
0034174859
-
Tamoxifen-induced hot flashes
-
(b) Loprinzi, C. L.; Zahasky, K. M.; Slaoan, J. A.; Novotny, P. J.; Quella, S. K. Tamoxifen-Induced Hot Flashes. Clin. Breast Cancer 2000, 1, 52-56.
-
(2000)
Clin. Breast Cancer
, vol.1
, pp. 52-56
-
-
Loprinzi, C.L.1
Zahasky, K.M.2
Slaoan, J.A.3
Novotny, P.J.4
Quella, S.K.5
-
19
-
-
33744816435
-
-
Preparation of tetracyclic heterocycles as selective estrogen receptor modulators (SERMs) WO 2003053977, 2003. US 71997520031121, 2004
-
Kanojia, R. M.; Jain, N. F.; Ng, R.; Sui, Z.; Xu, J. Preparation of tetracyclic heterocycles as selective estrogen receptor modulators (SERMs) WO 2003053977, 2003. US 71997520031121, 2004.
-
-
-
Kanojia, R.M.1
Jain, N.F.2
Ng, R.3
Sui, Z.4
Xu, J.5
-
20
-
-
3242810437
-
Preparation of tetracyclic heterocycles as selective estrogen receptor modulators (SERMs)
-
For synthesis of the tetracyclic core structure, see (a) Kanojia, R. M.; Jain, N.; Xu, J.; Sui, Z. Preparation of tetracyclic heterocycles as selective estrogen receptor modulators (SERMs). Tetrahedron Lett. 2004, 45, 5837-5839.
-
(2004)
Tetrahedron Lett.
, vol.45
, pp. 5837-5839
-
-
Kanojia, R.M.1
Jain, N.2
Xu, J.3
Sui, Z.4
-
21
-
-
28644446613
-
A novel approach to the synthesis of 11,11-diinethyl-bisbenzopyran-5-ones
-
(b) Jain, N.; Xu, J.; Chen, N.; Sui, Z. A novel approach to the synthesis of 11,11-diinethyl-bisbenzopyran-5-ones. Tetrahedron Lett. 2006, 47, 225-228.
-
(2006)
Tetrahedron Lett.
, vol.47
, pp. 225-228
-
-
Jain, N.1
Xu, J.2
Chen, N.3
Sui, Z.4
-
22
-
-
33744804499
-
-
note
-
(a) The absolute configuration of 1-(R) and 1-(S) has been determined by VCD spectroscopy data.
-
-
-
-
23
-
-
33744802570
-
-
note
-
(b) ee values were > 95; optical purities were determined by chiral Pak AD column.
-
-
-
-
24
-
-
0033571579
-
An ultrahigh-throughput screening assay for estrogen receptor ligands
-
Allan, G. F.; Hutchins, A.; Clancy, J. An ultrahigh-throughput screening assay for estrogen receptor ligands. Anal. Biochem. 1999, 275, 243-247.
-
(1999)
Anal. Biochem.
, vol.275
, pp. 243-247
-
-
Allan, G.F.1
Hutchins, A.2
Clancy, J.3
-
25
-
-
0037090988
-
Characterization of selective estrogen receptor modulator (SERM) activity in two triarylethylene oxybutyric acids
-
(b) Rufbin, V. N.; Ruenitz, P. C.; Boyd, J. L.; Boudinot, F. D.; Wiese, T. E. Characterization of Selective Estrogen Receptor Modulator (SERM) Activity in Two Triarylethylene Oxybutyric Acids. Biochem. Pharmacol. 2002, 63, 1517-1525.
-
(2002)
Biochem. Pharmacol.
, vol.63
, pp. 1517-1525
-
-
Rufbin, V.N.1
Ruenitz, P.C.2
Boyd, J.L.3
Boudinot, F.D.4
Wiese, T.E.5
-
26
-
-
0029947174
-
Molecular effects of genistein on estrogen receptor mediated pathways
-
Wang, T. T.; Sathyamoorthy, N.; Phang, J. M. Molecular Effects of Genistein on Estrogen Receptor Mediated Pathways. Carcinogenesis 1996, 17, 271-275.
-
(1996)
Carcinogenesis
, vol.17
, pp. 271-275
-
-
Wang, T.T.1
Sathyamoorthy, N.2
Phang, J.M.3
-
27
-
-
33744803126
-
-
note
-
Possible path way for auto oxidation is described in ref 8b.
-
-
-
-
28
-
-
0022547861
-
Estrogen regulation of protein synthesis in the immature rat uterus: The analysis of proteins released into the medium during in vitro incubation
-
(a) Komm B. S.; Rusling D. J.; Lyttle C. R. Estrogen regulation of protein synthesis in the immature rat uterus: the analysis of proteins released into the medium during in vitro incubation. Endocrinology 1986, 118, 2411-2416.
-
(1986)
Endocrinology
, vol.118
, pp. 2411-2416
-
-
Komm, B.S.1
Rusling, D.J.2
Lyttle, C.R.3
-
29
-
-
23844531615
-
Bazedoxifene acetate: A selective estrogen receptor modulator with improved selectivity
-
(b) Komm, B. S.; Kharode, Y. P.; Bodine, P. V. N.; Harris, H. A.; Miller, C. P.; Lyttle, C. R. Bazedoxifene acetate: a selective estrogen receptor modulator with improved selectivity. Endocrinology 2005, 146 (9), 3999-4008.
-
(2005)
Endocrinology
, vol.146
, Issue.9
, pp. 3999-4008
-
-
Komm, B.S.1
Kharode, Y.P.2
Bodine, P.V.N.3
Harris, H.A.4
Miller, C.P.5
Lyttle, C.R.6
-
30
-
-
0035686794
-
Developing a SERM: Stringent preclinical selection criteria leading to an acceptable candidate (WAY-140424) for clinical evaluation
-
(a) Komm, B. S.; Lyttle, C. R. Developing a SERM: Stringent preclinical selection criteria leading to an acceptable candidate (WAY-140424) for clinical evaluation. Ann. N.Y. Acad. Sci. 2001, 949, 317-326.
-
(2001)
Ann. N.Y. Acad. Sci.
, vol.949
, pp. 317-326
-
-
Komm, B.S.1
Lyttle, C.R.2
-
31
-
-
0031171316
-
Activity of raloxifene in immature and ovariectomized rat uterotrophic assays
-
(b) Ashby J.; Odum, J.; Foster, J. R. Activity of raloxifene in immature and ovariectomized rat uterotrophic assays. Toxicol Pharmacol 1997, 25, 226-231.
-
(1997)
Toxicol Pharmacol
, vol.25
, pp. 226-231
-
-
Ashby, J.1
Odum, J.2
Foster, J.R.3
-
32
-
-
17744368482
-
Selective estrogenic effects of a novel triphenylethylene compound, FC1271a, on bone, cholesterol level, and reproductive tissues in intact and ovariectomized rats
-
(c) Qu, Q.; Zheng, H.; Dahllund, J.; Laine, A.; Cockcroft, N.; Peng, Z.; Koskinen, M.; Hemminki, K.; Kangas, L.; Väänänen, K.; Härkönen, P. Selective estrogenic effects of a novel triphenylethylene compound, FC1271a, on bone, cholesterol level, and reproductive tissues in intact and ovariectomized rats. Endocrinology 2000, 141, 809-820.
-
(2000)
Endocrinology
, vol.141
, pp. 809-820
-
-
Qu, Q.1
Zheng, H.2
Dahllund, J.3
Laine, A.4
Cockcroft, N.5
Peng, Z.6
Koskinen, M.7
Hemminki, K.8
Kangas, L.9
Väänänen, K.10
Härkönen, P.11
-
33
-
-
0032462194
-
U. J. LY353381.HCl: A novel raloxifene analogue with improved SERM potency and efficacy in vivo
-
(d) Sato, M.; Turner, C. H.; Wang, T.; Adrian, M. D.; Rowley, E.; Bryant, H. U. J. LY353381.HCl: a novel raloxifene analogue with improved SERM potency and efficacy in vivo. Pharmacol. Exp. Ther. 1998, 287, 1-7.
-
(1998)
Pharmacol. Exp. Ther.
, vol.287
, pp. 1-7
-
-
Sato, M.1
Turner, C.H.2
Wang, T.3
Adrian, M.D.4
Rowley, E.5
Bryant, H.6
-
34
-
-
24944563779
-
A new selective estrogen receptor modulator with potent uterine antagonist activity, agonist activity in bone, and minimal ovarian stimulation
-
Geiser, A. G.; Hummel, C. W.; Draper, M. W.; Henck, J. W.; Cohen, I. R.; Rudmann, D. G.; Donnelly, K. B.; Adrian, M. D.; Shepherd, T. A.; Wallace, O. B.; McCann, D. J.; Oldham, S. W.; Bryant, H. U.; Sato, M.; Dodge, J. A. A new selective estrogen receptor modulator with potent uterine antagonist activity, agonist activity in bone, and minimal ovarian stimulation. Endocrinology 2005, 146 (10), 4524-4535.
-
(2005)
Endocrinology
, vol.146
, Issue.10
, pp. 4524-4535
-
-
Geiser, A.G.1
Hummel, C.W.2
Draper, M.W.3
Henck, J.W.4
Cohen, I.R.5
Rudmann, D.G.6
Donnelly, K.B.7
Adrian, M.D.8
Shepherd, T.A.9
Wallace, O.B.10
McCann, D.J.11
Oldham, S.W.12
Bryant, H.U.13
Sato, M.14
Dodge, J.A.15
-
35
-
-
0020530703
-
Chronic hyperprolactinemia reduces peripheral beta-adrenergic responsiveness in male rats
-
(a) Simpkins, J. W.; Katovich, M. J.; Song, I.-C. Chronic hyperprolactinemia reduces peripheral beta-adrenergic responsiveness in male rats. Life Sci. 1983, 32, 1957-1966.
-
(1983)
Life Sci.
, vol.32
, pp. 1957-1966
-
-
Simpkins, J.W.1
Katovich, M.J.2
Song, I.-C.3
-
36
-
-
0022602272
-
Regional skin temperature changes in a rat model for the menopausal hot flush
-
(b) Katovich, M. J.; Simpkins, J. W.; Berglund, L. A.; O'Meara, J. Regional skin temperature changes in a rat model for the menopausal hot flush. Maturitas 1986, 8, 67-76.
-
(1986)
Maturitas
, vol.8
, pp. 67-76
-
-
Katovich, M.J.1
Simpkins, J.W.2
Berglund, L.A.3
O'Meara, J.4
-
37
-
-
0032538822
-
The effect of estrogens and antiestrogens in a rat model for hot flush
-
(c) Merchenthaler, I.; Funkhouser, J. M.; Carver, J. M.; Lundeen, S. G.; Ghosh, K.; Winneker, R. C. The effect of estrogens and antiestrogens in a rat model for hot flush. Maturitas 1998, 30, 307-316.
-
(1998)
Maturitas
, vol.30
, pp. 307-316
-
-
Merchenthaler, I.1
Funkhouser, J.M.2
Carver, J.M.3
Lundeen, S.G.4
Ghosh, K.5
Winneker, R.C.6
-
38
-
-
33744824306
-
-
note
-
Both 1-(R) and 1-(S) have similar pharmacokinetic properties in rats. The active metabolites 2d-(R) and 2d-(S) were detected in plasma predominantly with similar exposures as compared to the parent compounds 1-(R) and 1-(S), respectively. The total bioavailability calculated for 1-(R) and 1-(S) was about 11% and 9%, respectively. The partial hydrolyzed products were not detected in rat plasma.
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-
-
-
39
-
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33744824865
-
-
note
-
(a) The concentration of these compounds in blood was not determined in the immature uterotropic assays.
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-
-
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40
-
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33744821574
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-
note
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(b) From our PK study, we have shown that 1-(R) and 1-(S) are extensively metabolized to 2d-(R) and 2d-(S), respectively. To correct the molecular weight change, a 1.4 mg/kg dose was chosen as standard screening dose.
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-
-
-
41
-
-
33744822405
-
Selective estrogen receptor modulators
-
Matsumoto, T.; Morii, H.; Yazaki, Y.; Ouchi, Y., Eds.
-
(a) Matsumoto, T.; Morii, H.; Yazaki, Y.; Ouchi, Y., Eds. Selective Estrogen Receptor Modulators. Clin. Calcium 2002, 12 (12), 102 pp.
-
(2002)
Clin. Calcium
, vol.12
, Issue.12
, pp. 102
-
-
-
42
-
-
0030071445
-
Tripartite steroid hormone receptor pharmacology: Interaction with multiple effector sites as a basis for the cell- and promoter-specific action of these hormones
-
(b) For a detailed description of the current understanding of tissue-specific steroid hormone activities, see Katzenellenbogen, J. A.; O'Malley, B. W.; Katzenellenbogen, B. S. Tripartite steroid hormone receptor pharmacology: Interaction with multiple effector sites as a basis for the cell- and promoter-specific action of these hormones. Mol. Endocrinol. 1996, 10, 119-131.
-
(1996)
Mol. Endocrinol.
, vol.10
, pp. 119-131
-
-
Katzenellenbogen, J.A.1
O'Malley, B.W.2
Katzenellenbogen, B.S.3
-
43
-
-
33744798968
-
-
note
-
See Supporting Information for details.
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