메뉴 건너뛰기




Volumn 49, Issue 3, 2006, Pages 843-846

A selective estrogen receptor modulator for the treatment of hot flushes

Author keywords

[No Author keywords available]

Indexed keywords

6 HYDROXY 2 (4 HYDROXYPHENYL) 3 [4 [2 (1 PYRROLIDINYL)ETHOXY]BENZOYL]BENZO[B]THIOPHENE; 7,9 DIFLUORO 5 [4 (2 PIPERIDIN 1 YLETHOXY)PHENYL] 5H 6 OXCHRYSEN 2 OL; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR ALPHA ANTAGONIST; ESTROGEN RECEPTOR BETA; ESTROGEN RECEPTOR BETA ANTAGONIST; LSN 2120310; RALOXIFENE; SELECTIVE ESTROGEN RECEPTOR MODULATOR; TAMOXIFEN; UNCLASSIFIED DRUG;

EID: 32344433109     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm0509795     Document Type: Article
Times cited : (38)

References (24)
  • 1
    • 0000880169 scopus 로고
    • Menopausal symptoms in women of various ages
    • Neugarten, B. L.; Kraines, R. J. Menopausal symptoms in women of various ages. Psychosom. Med. 1965, 27, 266-273.
    • (1965) Psychosom. Med. , vol.27 , pp. 266-273
    • Neugarten, B.L.1    Kraines, R.J.2
  • 2
    • 0000576628 scopus 로고
    • The perimenopausal symptoms: The statistical analysis of a survey
    • Jaszmann, L.; Van Lith, N. D.; Zaat, J. C. A. The perimenopausal symptoms: The statistical analysis of a survey. Med Gynecol. Socio. 1969, 4, 268-277.
    • (1969) Med Gynecol. Socio. , vol.4 , pp. 268-277
    • Jaszmann, L.1    Van Lith, N.D.2    Zaat, J.C.A.3
  • 3
    • 0023204660 scopus 로고
    • Thermoregulatory physiology of menopausal hot flashes: A review
    • Kronenberg, F.; Downey, J. A. Thermoregulatory physiology of menopausal hot flashes: a review. Can. J. Physiol. Pharmacol. 1987, 65, 1312-1324.
    • (1987) Can. J. Physiol. Pharmacol. , vol.65 , pp. 1312-1324
    • Kronenberg, F.1    Downey, J.A.2
  • 6
    • 0030015080 scopus 로고    scopus 로고
    • A controlled trial of raloxifene (LY139481) HCl: Impact on bone turnover and serum lipid profile in healthy post-menopausal women
    • Draper, M. W.; Flowers, D. E.; Huster, W. J.; Neild, J. A.; Harper, K. D.; Arnaud, C. A controlled trial of raloxifene (LY139481) HCl: impact on bone turnover and serum lipid profile in healthy post-menopausal women. J. Bone Miner. Res. 1996, 11, 835-842.
    • (1996) J. Bone Miner. Res. , vol.11 , pp. 835-842
    • Draper, M.W.1    Flowers, D.E.2    Huster, W.J.3    Neild, J.A.4    Harper, K.D.5    Arnaud, C.6
  • 8
    • 0032547326 scopus 로고    scopus 로고
    • Randomized trial of estrogen plus progestin for secondary prevention of coronary heart disease in postmenopausal women
    • Hulley, S.; Grady, D.; Bush, T.; Furberg, C.; Herrington, D.; Riggs, B.; Vittinghoff, E. 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    Furberg, C.4    Herrington, D.5    Riggs, B.6    Vittinghoff, E.7
  • 9
    • 0026670057 scopus 로고
    • Can we improve compliance with long-term HRT?
    • Coope, J.; March, J. Can we improve compliance with long-term HRT? Maturitas 1992, 15, 151-158.
    • (1992) Maturitas , vol.15 , pp. 151-158
    • Coope, J.1    March, J.2
  • 10
    • 0141455199 scopus 로고    scopus 로고
    • Discovery and preclinical characterization of (+)-3-[4-(1- piperidinoethoxy)pnenyl]spiro[indene-1,1′-indane]-5,5′-diol hydrochloride: A promising nonsteroidal estrogen receptor agonist for hot flush
    • Watanabe, N.; Ikeno, A.; Minato, H.; Nakagawa, H.; Kohayakawa, C.; Tsuji, J-i. Discovery and preclinical characterization of (+)-3-[4-(1- piperidinoethoxy)pnenyl]spiro[indene-1,1′-indane]-5,5′-diol hydrochloride: a promising nonsteroidal estrogen receptor agonist for hot flush. J. Med. Chem. 2003, 46, 3961-3964.
    • (2003) J. Med. Chem. , vol.46 , pp. 3961-3964
    • Watanabe, N.1    Ikeno, A.2    Minato, H.3    Nakagawa, H.4    Kohayakawa, C.5    Tsuji, J.-I.6
  • 12
    • 0032541271 scopus 로고    scopus 로고
    • Reduction of carbonyl compounds with chiral oxazaborolidine catalysts: A new paradigm for enantioselective catalysis and a powerful new synthetic method
    • Corey, E. J.; Helal, C. J. Reduction of carbonyl compounds with chiral oxazaborolidine catalysts: a new paradigm for enantioselective catalysis and a powerful new synthetic method. Angew. Chem., Intl. Ed. 1998, 37, 1986.
    • (1998) Angew. Chem., Intl. Ed. , vol.37 , pp. 1986
    • Corey, E.J.1    Helal, C.J.2
  • 13
    • 32344436751 scopus 로고    scopus 로고
    • note
    • The absolute configuration was assigned based on an X-ray crystal structure of 1 bound to ERα.
  • 14
    • 0037718356 scopus 로고    scopus 로고
    • Tetrahydroquinoline-based selective estrogen receptor modulators (SERMs)
    • For a detailed description of the ER binding and MCF-7 assay protocols, see: Wallace, O. B.; Lauwers, K. S.; Jones, S. A.; Dodge, J. A. Tetrahydroquinoline-based selective estrogen receptor modulators (SERMs). Bioorg. Med. Chem. Lett. 2003, 13, 1907-1910.
    • (2003) Bioorg. Med. Chem. Lett. , vol.13 , pp. 1907-1910
    • Wallace, O.B.1    Lauwers, K.S.2    Jones, S.A.3    Dodge, J.A.4
  • 15
    • 4544314485 scopus 로고    scopus 로고
    • Benzothiophene and naphthalene derived constrained SERMs
    • For a detailed description of the Ishikawa assay protocol, see: Wallace, O. B.; Bryant, H. U.; Shetler, P. K.; Adrian, M. D.; Geiser, A. G. Benzothiophene and naphthalene derived constrained SERMs. Bioorg. Med. Chem. Lett. 2004, 14, 5103-5106.
    • (2004) Bioorg. Med. Chem. Lett. , vol.14 , pp. 5103-5106
    • Wallace, O.B.1    Bryant, H.U.2    Shetler, P.K.3    Adrian, M.D.4    Geiser, A.G.5
  • 16
    • 2442464650 scopus 로고
    • Uterine peroxidase as a marker for estrogen action
    • Lyttle, C. R.; DeSombre, E. R. Uterine peroxidase as a marker for estrogen action. Proc. Natl. Acad. Sci. U.S.A. 1977, 74, 3162-3166.
    • (1977) Proc. Natl. Acad. Sci. U.S.A. , vol.74 , pp. 3162-3166
    • Lyttle, C.R.1    DeSombre, E.R.2
  • 17
    • 0027143193 scopus 로고
    • Molecular structures, conformational analysis, and preferential modes of binding of 3-aroyl-2-arylbenzo[b]thiophene estrogen receptor ligands: LY117018 and aryl azide photoaffinity labeling analogues
    • Kym P. R.; Anstead G. M.; Pinney K. G.; Wilson, S. R.; Katzenellenbogen J. A. Molecular structures, conformational analysis, and preferential modes of binding of 3-aroyl-2-arylbenzo[b]thiophene estrogen receptor ligands: LY117018 and aryl azide photoaffinity labeling analogues. J. Med. Chem. 1993, 36, 3910-3922.
    • (1993) J. Med. Chem. , vol.36 , pp. 3910-3922
    • Kym, P.R.1    Anstead, G.M.2    Pinney, K.G.3    Wilson, S.R.4    Katzenellenbogen, J.A.5
  • 18
    • 0031799147 scopus 로고    scopus 로고
    • The preventive and interventional effects of raloxifene analogue (LY117018 HCl) on osteopenia in ovariectomized rats
    • (b) Li, X.; Takahashi, M.; Kushida, K.; Inoue, T. The preventive and interventional effects of raloxifene analogue (LY117018 HCl) on osteopenia in ovariectomized rats. J. Bone Min. Res. 1998,13, 1005-1010.
    • (1998) J. Bone Min. Res. , vol.13 , pp. 1005-1010
    • Li, X.1    Takahashi, M.2    Kushida, K.3    Inoue, T.4
  • 20
    • 0021201213 scopus 로고
    • Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4- hydroxyphenyl)benzo[b]thien-3-yl]-[4-[2-(1-piperidinyl)ethoxy]-phenyl] -methanone hydrochloride (LY 156758), a remarkably effective estrogen antagonist with only minimal intrinsic estrogenicity
    • (d) 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 series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl]-[4-[2- (1-piperidinyl)ethoxy]-phenyl]-methanone hydrochloride (LY 156758), 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
  • 21
    • 0021091890 scopus 로고
    • Comparison of the biological effects of tamoxifen and a new antiestrogen (LY 117018) on the immature rat uterus
    • (e) Wakeling, A. E.; O'Connor, K. M.; Newboult, E. Comparison of the biological effects of tamoxifen and a new antiestrogen (LY 117018) on the immature rat uterus. J. Endocrinol. 1983, 99, 447-453.
    • (1983) J. Endocrinol. , vol.99 , pp. 447-453
    • Wakeling, A.E.1    O'Connor, K.M.2    Newboult, E.3
  • 22
    • 0020583948 scopus 로고
    • Similarities between morphine withdrawal in the rat and the menopausal hot flush
    • Simpkins, J. W.; Katovich, M. J.; Song, I.-C. Similarities between morphine withdrawal in the rat and the menopausal hot flush. 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
  • 24
    • 0035686794 scopus 로고    scopus 로고
    • Developing a SERM: Stringent preclinical selection criteria leading to an acceptable candidate (WAY-140424) for clinical evaluation
    • (c) Komm, B. S.; Lyttle, C. R. Developing a SERM: Stringent preclinical selection criteria leading to an acceptable candidate (WAY-140424) for clinical evaluation. Ann. NY Acad. Sci. 2001, 949, 317-326.
    • (2001) Ann. NY Acad. Sci. , vol.949 , pp. 317-326
    • Komm, B.S.1    Lyttle, C.R.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.