-
1
-
-
77956727943
-
Estrogen receptor modulators: Effects in non-traditional target tissues
-
Bristol, J. A., Ed.; Academic Press: New York
-
Grese, T. A.; Dodge, J. A. Estrogen receptor modulators: effects in non-traditional target tissues. In Annual Reports in Medicinal Chemistry; Bristol, J. A., Ed.; Academic Press: New York, 1996; Vol. 31, pp 181-190.
-
(1996)
Annual Reports in Medicinal Chemistry
, vol.31
, pp. 181-190
-
-
Grese, T.A.1
Dodge, J.A.2
-
2
-
-
0029038986
-
Analysis of estrogen receptor function in vitro reveals three distinct classes of antiestrogens
-
(a) McDonnell, D. P.; Clemm, D. L.; Hermann, T.; Goldman, M. E.; Pike, J. W. Analysis of estrogen receptor function in vitro reveals three distinct classes of antiestrogens. Mol. Endocrinol. 1995, 9, 659-669.
-
(1995)
Mol. Endocrinol.
, vol.9
, pp. 659-669
-
-
McDonnell, D.P.1
Clemm, D.L.2
Hermann, T.3
Goldman, M.E.4
Pike, J.W.5
-
3
-
-
0029560877
-
Selective estrogen receptor modulators
-
(b) Kauffman, R. F.; Bryant, H. U. Selective estrogen receptor modulators. Drug News Perspect. 1995, 8, 531-539.
-
(1995)
Drug News Perspect
, vol.8
, pp. 531-539
-
-
Kauffman, R.F.1
Bryant, H.U.2
-
4
-
-
0029994748
-
Raloxifene, tamoxifen, nafoxidine, or estrogen effects on reproductive and nonreproductive tissues in ovariectomized rats
-
(c) Sato, M.; Rippy, M. K.; Bryant, H. U. Raloxifene, tamoxifen, nafoxidine, or estrogen effects on reproductive and nonreproductive tissues in ovariectomized rats. FASEB J. 1996, 10, 905-912.
-
(1996)
FASEB J.
, vol.10
, pp. 905-912
-
-
Sato, M.1
Rippy, M.K.2
Bryant, H.U.3
-
5
-
-
0026395885
-
A potent specific pure antiestrogen with clinical potential
-
(a) Wakeling, A. E.; Dukes, M.; Bowler, J. A potent specific pure antiestrogen with clinical potential. Cancer Res. 1991, 51, 3867-3873.
-
(1991)
Cancer Res.
, vol.51
, pp. 3867-3873
-
-
Wakeling, A.E.1
Dukes, M.2
Bowler, J.3
-
6
-
-
0027139169
-
The estrogen antagonist ICI 182780 reduces cancellous bone volume in female rats
-
(b) Gallagher A.; Chambers, T. J.; Tobias, J. H. The estrogen antagonist ICI 182780 reduces cancellous bone volume in female rats. Endocrinology 1993, 133, 835-842.
-
(1993)
Endocrinology
, vol.133
, pp. 835-842
-
-
Gallagher, A.1
Chambers, T.J.2
Tobias, J.H.3
-
7
-
-
0001292133
-
Selective estrogen receptor modulators: Pharmacological profile in the rat uterus
-
(c) Bryant, H. U.; Wilson, P. K.; Adrian, M. D.; Cole, H. W.; Phillips, D. L.; Dodge, J. A.; Grese, T. A.; Sluka, J. P.; Glasebrook, A. L. Selective estrogen receptor modulators: pharmacological profile in the rat uterus. J. Soc. Gynecol. Invest. 1998, 3, 152A.
-
(1998)
J. Soc. Gynecol. Invest.
, vol.3
-
-
Bryant, H.U.1
Wilson, P.K.2
Adrian, M.D.3
Cole, H.W.4
Phillips, D.L.5
Dodge, J.A.6
Grese, T.A.7
Sluka, J.P.8
Glasebrook, A.L.9
-
8
-
-
0028167482
-
Raloxifene (LY139481 HCl) prevents bone loss and reduces serum cholesterol without causing uterine hypertrophy in ovariectomized rats
-
(a) Black, L. J.; Sato, M.; Rowley, E. R.; Magee, D. E.; Bekele, A.; Williams, D. C.; Cullinan, G. J.; Bendele, R.; Kauffmann, R. F.; Bensch, W. R.; Frolik, C. A.; Termine, J. D.; Bryant, H. U. Raloxifene (LY139481 HCl) prevents bone loss and reduces serum cholesterol without causing uterine hypertrophy in ovariectomized rats. J Clin. Invest. 1994, 93, 63-69.
-
(1994)
J Clin. Invest.
, vol.93
, pp. 63-69
-
-
Black, L.J.1
Sato, M.2
Rowley, E.R.3
Magee, D.E.4
Bekele, A.5
Williams, D.C.6
Cullinan, G.J.7
Bendele, R.8
Kauffmann, R.F.9
Bensch, W.R.10
Frolik, C.A.11
Termine, J.D.12
Bryant, H.U.13
-
9
-
-
0030015080
-
A controlled trial of raloxifene (LY139481 HCl): Impact on bone turnover and serum lipid profile in healthy postmenopausal women
-
(b) Draper, M. W.; Flowers, D. E.; Huster, W. J.; Nield, J. A.; Harper, K. D.; Arnaud, C. A controlled trial of raloxifene (LY139481 HCl): Impact on bone turnover and serum lipid profile in healthy postmenopausal women. J. Bone Mineral Res. 1996, 11, 835-842.
-
(1996)
J. Bone Mineral Res.
, vol.11
, pp. 835-842
-
-
Draper, M.W.1
Flowers, D.E.2
Huster, W.J.3
Nield, J.A.4
Harper, K.D.5
Arnaud, C.6
-
10
-
-
0019122379
-
Pharmacology of tamoxifen in laboratory animals
-
(c) Jordan, V. C.; Allen, K. E.; Dix, C. J. Pharmacology of tamoxifen in laboratory animals. Cancer Treat. Rep. 1980, 64, 745-759.
-
(1980)
Cancer Treat. Rep.
, vol.64
, pp. 745-759
-
-
Jordan, V.C.1
Allen, K.E.2
Dix, C.J.3
-
11
-
-
0027172047
-
A current view of tamoxifen for the treatment and prevention of breast cancer
-
(d) Jordan, V. C. A current view of tamoxifen for the treatment and prevention of breast cancer. Br. J. Pharmacol. 1993, 110, 507-517.
-
(1993)
Br. J. Pharmacol.
, vol.110
, pp. 507-517
-
-
Jordan, V.C.1
-
12
-
-
0002447973
-
Sex steroids in the pathogenesis and prevention of osteoporosis
-
Riggs, B. L., Melton, L. J., Eds.; Raven: New York
-
(e) Lindsay, R. Sex steroids in the pathogenesis and prevention of osteoporosis. In Osteoporosis: Etiology, Diagnosis, and Management; Riggs, B. L., Melton, L. J., Eds.; Raven: New York, 1988; pp 333-358.
-
(1988)
Osteoporosis: Etiology, Diagnosis, and Management
, pp. 333-358
-
-
Lindsay, R.1
-
13
-
-
0028919090
-
Estrogen receptors in human nontarget tissues: Biological and clinical implications
-
(f) Ciocca, D. R.; Vargas Roig, L. M. Estrogen receptors in human nontarget tissues: biological and clinical implications. Endocr. Rev. 1995, 16, 35-62.
-
(1995)
Endocr. Rev.
, vol.16
, pp. 35-62
-
-
Ciocca, D.R.1
Vargas Roig, L.M.2
-
14
-
-
0027476353
-
Current concepts in estrogen replacement therapy in the menopause
-
(g) Session, D. R.; Kelley, A. C.; Jewelewicz, R. Current concepts in estrogen replacement therapy in the menopause. Fertility Sterility 1993, 2, 277-284.
-
(1993)
Fertility Sterility
, vol.2
, pp. 277-284
-
-
Session, D.R.1
Kelley, A.C.2
Jewelewicz, R.3
-
15
-
-
0029056755
-
The use of estrogens and progestins and the risk of breast cancer in postmenopausal women
-
(h) Colditz, G. A.; Hankinson, S. E.; Hunter, D. J.; Willett, W. C.; Manson, J. E.; Stampfer, M. J.; Hennekens, C.; Rosner, B.; Speizer, F. E. The use of estrogens and progestins and the risk of breast cancer in postmenopausal women. N. Engl. J. Med. 1995, 332, 1589-1593.
-
(1995)
N. Engl. J. Med.
, vol.332
, pp. 1589-1593
-
-
Colditz, G.A.1
Hankinson, S.E.2
Hunter, D.J.3
Willett, W.C.4
Manson, J.E.5
Stampfer, M.J.6
Hennekens, C.7
Rosner, B.8
Speizer, F.E.9
-
16
-
-
0013666830
-
Raloxifene causes rapid regression of abdominal wall leiomyomas in the estrogen-induced guinea pig model
-
(i) Porter, K. B.; Tsibris, J. C. M.; Porter, G. W.; Fuchs-Young, R.; O'Brien, W. F.; Knadler, M. P.; Spellacy, W. N. Raloxifene causes rapid regression of abdominal wall leiomyomas in the estrogen-induced guinea pig model. J, Soc. Gynecol. Invest. 1996, 3, 147A.
-
(1996)
J, Soc. Gynecol. Invest.
, vol.3
-
-
Porter, K.B.1
Tsibris, J.C.M.2
Porter, G.W.3
Fuchs-Young, R.4
O'Brien, W.F.5
Knadler, M.P.6
Spellacy, W.N.7
-
17
-
-
0020582094
-
Effects of a new antiestrogen, keoxifene (LY156758), on growth of carcinogen-induced mammary tumors on LH and prolactin levels
-
Clemens, J. A.; Bennett, D. R.; Black, L. J.; Jones, C. D. Effects of a new antiestrogen, keoxifene (LY156758), on growth of carcinogen-induced mammary tumors on LH and prolactin levels. Life Sci. 1983, 32, 2869-2875.
-
(1983)
Life Sci.
, vol.32
, pp. 2869-2875
-
-
Clemens, J.A.1
Bennett, D.R.2
Black, L.J.3
Jones, C.D.4
-
18
-
-
0030071445
-
Tripartite steroid hormone receptor pharmacology: Interaction with multiple effector sites as basis for the cell- and promoter-specific action of these hormones
-
Katzenellenbogen, J. A.; O'Malley, B. W.; Katzenellenbogen, B. S. Tripartite steroid hormone receptor pharmacology: Interaction with multiple effector sites as 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
-
19
-
-
0023625418
-
Evidence that transforming growth facotr-beta is a hormonally regulated negative growth factor in human breast cancer cells
-
(a) Knabbe, C.; Lippman, M. E.; Wakefield, L. M.; Flanders, K. C.; Kasid, A.; Derynck, R.; Dickon, R. B. Evidence that transforming growth facotr-beta is a hormonally regulated negative growth factor in human breast cancer cells. Cell 1987, 48, 417-428.
-
(1987)
Cell
, vol.48
, pp. 417-428
-
-
Knabbe, C.1
Lippman, M.E.2
Wakefield, L.M.3
Flanders, K.C.4
Kasid, A.5
Derynck, R.6
Dickon, R.B.7
-
20
-
-
0025113699
-
Anti-estrogens induce the secretion of active transforming growth factor beta from human fetal fibroblasts
-
(b) Colletta, A. A.; Wakefield, L. M.; Howell, F. V.; van Roozendaal, K. E. P.; Danielpour, D.; Ebbs, S. R.; Sporn, M. B.; Baum, M. Anti-estrogens induce the secretion of active transforming growth factor beta from human fetal fibroblasts. Br. J. Cancer 1990, 62, 405-409.
-
(1990)
Br. J. Cancer
, vol.62
, pp. 405-409
-
-
Colletta, A.A.1
Wakefield, L.M.2
Howell, F.V.3
Van Roozendaal, K.E.P.4
Danielpour, D.5
Ebbs, S.R.6
Sporn, M.B.7
Baum, M.8
-
21
-
-
0029961569
-
Estrogen and raloxifene stimulate transforming growth factor beta-3 (TGF-b3) gene expression in rat bone: A potential mechanism for estrogen and raloxifene mediated bone maintenance
-
(c) Yang, N. N.; Bryant, H. U.; Hardikar, S.; Sato, M.; Galvin, R.; Glasebrook, A. L. Estrogen and raloxifene stimulate transforming growth factor beta-3 (TGF-b3) gene expression in rat bone: a potential mechanism for estrogen and raloxifene mediated bone maintenance. Endocrinology 1996, 137, 2075-2081.
-
(1996)
Endocrinology
, vol.137
, pp. 2075-2081
-
-
Yang, N.N.1
Bryant, H.U.2
Hardikar, S.3
Sato, M.4
Galvin, R.5
Glasebrook, A.L.6
-
22
-
-
0029841146
-
Identification of an estrogen response element activated by metabolites of 17-β estradiol and raloxifene
-
Yang, N. N.; Venugopalan, M.; Hardikar, S.; Glasebrook, A. L. Identification of an estrogen response element activated by metabolites of 17-β estradiol and raloxifene. Science 1996, 273, 1222-1225.
-
(1996)
Science
, vol.273
, pp. 1222-1225
-
-
Yang, N.N.1
Venugopalan, M.2
Hardikar, S.3
Glasebrook, A.L.4
-
23
-
-
0021201213
-
Antiestrogens. 2. Structure-activity studies in a sereis of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thiene-3-yl][4-[2-(1-piperidinyl)-ethoxy] phenyl]methanone hydrochloride (LY156758), a remarkably effective estrogen antagonist with only minimal intrinsic estrogenicity
-
(a) Jones, C. D.; Jevnikar, M. G.; Pike, A. J.; Peters, M. K.; Black, L. J.; Thompson, A. R.; Falcone, J. F.; Clemens, J. A. Antiestrogens. 2. Structure-activity studies in a sereis of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thiene-3-yl][4-[2-(1-piperidinyl)-ethoxy] phenyl]methanone hydrochloride (LY156758), a remarkably effective estrogen antagonist with only minimal intrinsic estrogenicity. J. Med. Chem. 1984, 27, 1057-1066.
-
(1984)
J. Med. Chem.
, vol.27
, pp. 1057-1066
-
-
Jones, C.D.1
Jevnikar, M.G.2
Pike, A.J.3
Peters, M.K.4
Black, L.J.5
Thompson, A.R.6
Falcone, J.F.7
Clemens, J.A.8
-
24
-
-
15644370745
-
Structure-activity relationships of selective estrogen receptor modulators (SERMs). Modifications to the 2-arylbenzothiophene core of raloxifene
-
in press
-
(b) Grese, T. A.; Cho, S.; Finely, D. R.; Godfrey, A. G.; Jones, C. D.; Lugar, C. W., III; Martin, M. J.; Matsumoto, K.; Pennington, L. D.; Winter, M. A.; Adrian, M. D.; Cole, H. W.; Magee, D. E.; Phillips, D. L.; Rowley, E. R.; Short, L. L.; Glasebrook, A. L.; Bryant, H. U. Structure-activity relationships of selective estrogen receptor modulators (SERMs). Modifications to the 2-arylbenzothiophene core of raloxifene. J. Med. Chem., in press.
-
J. Med. Chem.
-
-
Grese, T.A.1
Cho, S.2
Finely, D.R.3
Godfrey, A.G.4
Jones, C.D.5
Lugar III, C.W.6
Martin, M.J.7
Matsumoto, K.8
Pennington, L.D.9
Winter, M.A.10
Adrian, M.D.11
Cole, H.W.12
Magee, D.E.13
Phillips, D.L.14
Rowley, E.R.15
Short, L.L.16
Glasebrook, A.L.17
Bryant, H.U.18
-
26
-
-
0000057992
-
Peroxytriflouroacetic acid. A convenient reagent for the preparation of sulfoxides and sulfones
-
Venier, C. G.; Squires, T. G.; Chen, Y.; Hussmann, G. P.; Shei, J. C.; Smith, B. F. Peroxytriflouroacetic acid. A convenient reagent for the preparation of sulfoxides and sulfones. J. Org. Chem. 1982, 47, 3773-3774.
-
(1982)
J. Org. Chem.
, vol.47
, pp. 3773-3774
-
-
Venier, C.G.1
Squires, T.G.2
Chen, Y.3
Hussmann, G.P.4
Shei, J.C.5
Smith, B.F.6
-
27
-
-
15644365670
-
-
note
-
2, 10% Pd/C, EtOH/EtOAc).
-
-
-
-
28
-
-
15644370958
-
-
Yield of 9a is overall from hydroxyphenyl disulfide
-
(b) Yield of 9a is overall from hydroxyphenyl disulfide.
-
-
-
-
29
-
-
33947332318
-
Selective reductions IX. Reactions of lithium aluminum hydride with selected organic compounds containing representative functional groups
-
Brown, H. C.; Weissman, P. M.; Min-Yoon, N. Selective reductions IX. Reactions of lithium aluminum hydride with selected organic compounds containing representative functional groups. J. Am. Chem. Soc. 1966, 88, 1458-1463.
-
(1966)
J. Am. Chem. Soc.
, vol.88
, pp. 1458-1463
-
-
Brown, H.C.1
Weissman, P.M.2
Min-Yoon, N.3
-
30
-
-
0019165813
-
A general synthesis of 6-H-pyrido[4,3-b]carbazole alkaloides
-
Miller, R. B.; Moock, T. A general synthesis of 6-H-pyrido[4,3-b]carbazole alkaloides. Tetrahedron Lett. 1980, 21, 3319-3322 and references cited therein.
-
(1980)
Tetrahedron Lett.
, vol.21
, pp. 3319-3322
-
-
Miller, R.B.1
Moock, T.2
-
31
-
-
0020516248
-
Antiestrogenic effects of LY117018 in MCF-7 cells
-
(a) Scholl, S. M.; Huff, K. K.; Lippman, M. E. Antiestrogenic effects of LY117018 in MCF-7 cells. Endocrinology 1983, 113, 611-617.
-
(1983)
Endocrinology
, vol.113
, pp. 611-617
-
-
Scholl, S.M.1
Huff, K.K.2
Lippman, M.E.3
-
32
-
-
0020569987
-
Characterization and quantitation of antiestrogen binding sites in estrogen receptor-positive and-negative human breast cancer cell lines
-
(b) Miller, M. A.; Katzenellenbogen, B. S. Characterization and quantitation of antiestrogen binding sites in estrogen receptor-positive and-negative human breast cancer cell lines. Cancer Res. 1983, 43, 3094-3100.
-
(1983)
Cancer Res.
, vol.43
, pp. 3094-3100
-
-
Miller, M.A.1
Katzenellenbogen, B.S.2
-
33
-
-
0024210084
-
Differential growth and invasiveness of MCF-7 breast cancer cells by antiestrogens
-
(c) Thompson, E. W.; Reich, R.; Shima, T. B.; Albini, A.; Graf, J.; Martin, G. R.; Dickson, R. B.; Lippman, M. E. Differential growth and invasiveness of MCF-7 breast cancer cells by antiestrogens. Cancer Res. 1988, 48, 6764-6768.
-
(1988)
Cancer Res.
, vol.48
, pp. 6764-6768
-
-
Thompson, E.W.1
Reich, R.2
Shima, T.B.3
Albini, A.4
Graf, J.5
Martin, G.R.6
Dickson, R.B.7
Lippman, M.E.8
-
34
-
-
0020694796
-
Antagonism of estrogen action with a new benzothiophene derived antiestrogen
-
Black, L. J.; Jones, C. D.; Falcone, J. F. Antagonism of estrogen action with a new benzothiophene derived antiestrogen. Life Sci. 1983, 32, 1031-1036.
-
(1983)
Life Sci.
, vol.32
, pp. 1031-1036
-
-
Black, L.J.1
Jones, C.D.2
Falcone, J.F.3
-
35
-
-
0028951607
-
Longitudinal and cross-sectional analysis of raloxifene effects on tibae from ovariectomized aged rats
-
(a) Sato, M.; Kim, J.; Short, L. L.; Slemenda, C. W.; Bryant, H. U. Longitudinal and cross-sectional analysis of raloxifene effects on tibae from ovariectomized aged rats. J. Pharmacol. Exp. Ther. 1995, 272, 1252-1259.
-
(1995)
J. Pharmacol. Exp. Ther.
, vol.272
, pp. 1252-1259
-
-
Sato, M.1
Kim, J.2
Short, L.L.3
Slemenda, C.W.4
Bryant, H.U.5
-
36
-
-
0343209783
-
Pharmacologic profile of estrogen induced uterine eosinophilia in the ovariectomized (OVX) rat
-
(b) Bryant, H. U.; Bendele, A. M.; Magee, D. E.; Cole, H. W.; Spaethe, S. W. Pharmacologic profile of estrogen induced uterine eosinophilia in the ovariectomized (OVX) rat. Pharmacologist 1992, 34, 194.
-
(1992)
Pharmacologist
, vol.34
, pp. 194
-
-
Bryant, H.U.1
Bendele, A.M.2
Magee, D.E.3
Cole, H.W.4
Spaethe, S.W.5
-
37
-
-
0019913863
-
-
Tamoxifen was purchased from Sigma Chemical Co., St. Louis, MO. 4-Hydroxytamoxifen was prepared at Lilly Research Laboratories according to procedures described in Robertson, D. W.; Katzenellenbogen, J. A. J. Org. Chem. 1982, 47, 2387-2393. ICI 182,780 was prepared at Lilly Research Laboratories according to the procedures described in Bowler, J.; Tait, B. S. U.S. Patent 4,659,516.
-
(1982)
J. Org. Chem.
, vol.47
, pp. 2387-2393
-
-
Robertson, D.W.1
Katzenellenbogen, J.A.2
-
38
-
-
0019913863
-
-
U.S. Patent 4,659,516
-
Tamoxifen was purchased from Sigma Chemical Co., St. Louis, MO. 4-Hydroxytamoxifen was prepared at Lilly Research Laboratories according to procedures described in Robertson, D. W.; Katzenellenbogen, J. A. J. Org. Chem. 1982, 47, 2387-2393. ICI 182,780 was prepared at Lilly Research Laboratories according to the procedures described in Bowler, J.; Tait, B. S. U.S. Patent 4,659,516.
-
-
-
Bowler, J.1
Tait, B.S.2
-
39
-
-
0029876149
-
Benzopyran selective estrogen receptor modulators (SERMs): Pharmacological effects and structural correlation with raloxifene
-
Grese, T. A.; Sluka, J. P.; Bryant, H. U.; Cole, H. W.; Kim, J. R.; Magee, D. E.; Rowley, E. R.; Sato, M. Benzopyran selective estrogen receptor modulators (SERMs): Pharmacological effects and structural correlation with raloxifene. Bioorg. Med. Chem. Lett. 1996, 6, 903-908.
-
(1996)
Bioorg. Med. Chem. Lett.
, vol.6
, pp. 903-908
-
-
Grese, T.A.1
Sluka, J.P.2
Bryant, H.U.3
Cole, H.W.4
Kim, J.R.5
Magee, D.E.6
Rowley, E.R.7
Sato, M.8
|