21
Views
5
CrossRef citations to date
0
Altmetric
Review

Selective oestrogen receptor modulators, pure antioestrogens and related oestrogen receptor ligands

Pages 337-353 | Published online: 02 Mar 2005

Bibliography

  • COSMAN F, LINDSAY R: Selective estrogen receptor modulators: clinical spectrum. Endocr: Rev (1999) 20:418–434.
  • MOSSELMAN S, POLMAN J, DIJKEMA R: ERP: identification and characterization of a novel human estrogen receptor. FEBS (1996) 392:49–53.
  • PETERSEN DN, TKALCEVIC GT, KOZA-TAYLOR PH, TURI TG, BROWN TA: Identification of estrogen receptor 132, a functional variant of estrogen receptor 13 expressed in normal rat tissues. Endocrinology (1998) 139:1082–1092.
  • HANSTEIN B, LIU H, YANCISIN MC, BROWN M: Functional analysis of a novel estrogen receptor-I3 isoform. Mol Endo. (1999) 13:129–137.
  • ZUMOFF B: Does postmenopausal estrogen administration increase the risk of breast cancer? Contributions of animal, biochemical, and clinical investigative studies to a resolution of the controversy. Proc. Soc. Exp. Biol. Med. (1998) 217:30–37.
  • WRITING GROUP FOR THE WOMEN'S HEALTH INITIATIVE INVESTIGATORS: Risks and benefits of estrogen plus progestin in healthy postmenopausal women. Principle results from the women's health initiative randomized controlled trial. JAMA (2002) 288:321–333.
  • BERESFORD SA, WEISS NS, VOIGT LK: Risk of endometrial cancer in relation to use of estrogen combined with cyclic progestin therapy in postmenopausal women. Lancet (1997) 349:458–461.
  • KAUFFMAN RE BRYANT HU: Selective estrogen receptor modulators. Drug News Perspect (1995) 8:531–539.
  • GRESE TA, DODGE JA: Selective estrogen receptor modulators (SERMs). Can: Pharm. Des. (1998) 4:71–92.
  • JORDAN VC: Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 2. Clinical considerations and new agents. J. Med. Chem. (2003) 46:1081–1111.
  • ••A very good review of the history andclinical applications of SERMs and ER modulators in general.
  • MEEGAN MJ, LLOYD DG: Advances in21. the science of estrogen receptor modulation. Carr. Med. Chem. (2003) 10:181–210.
  • ••This is a comprehensive review of the published ligands co-crystallised with both22.ER isoforms detailing the receptor-ligand interactions.
  • JORDAN VC: Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 1. Receptor interactions. J. Med. Chem. (2003) 46:883–908.
  • ••Comprehensive review of the ER structureand function, including a detailed discussion of the SERM mechanism of action.
  • MILLER CP: SERMs: evolutionary chemistry, revolutionary biology. Curl: Pharm. Des. (2002) 8:2089–2111.
  • KUIPER GGJM, CARLSSON B, GRANDIEN K et al: Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors a and P. Endocrinology (1997) 138:863–870.
  • GRESE TA, PENNINGTON LD, SLUKA JP et al.: Synthesis and pharmacology of conformationally restricted raloxifene analogues: highly potent selective estrogen receptor modulators. J. Med. Chem. (1998) 41:1272–1283.
  • STAUFFER SR, HUANG YR, ARON ZD et al.: Triarylpyrazoles with basic side chains: development of pyrazole-based estrogen receptor antagonists. Bioorg. Med. Chem. (2001) 9:151–161.
  • MILLER CP, COLLINI MD, TRAN BD et al.: Design, synthesis and preclinical characterization of novel, highly selective indole estrogens. J. Med. Chem. (2001) 44:1654–1657.
  • SCHMIDT JS, MERCURE J, TREMBLAY GB et al.: De novo design, synthesis and evaluation of novel nonsteroidal phenanthrene ligands for the estrogen receptor. J. Med. Chem. (2003) 46:1408–1418.
  • GRESE TA, ADRIAN MD, PHILLIPS DL et al.: Photochemical synthesis of N-arylbenzophenanthridine selective estrogen receptor modulators (SERMs). J. Med. Chem. (2001) 44:2857–2860.
  • SCHMIDT JS, MERCURE J, TREMBLAY GB et al.: De novo design, synthesis and evaluation of a novel non-steroidal diphenylnaphthyl ligand for the estrogen receptor. Bioorg. Med. Chem. (2003) 46:1389–1396.
  • HENKE BR, CONSLER TG, GO Net al.: A new series of estrogen receptor modulators that display selectivity for estrogen receptor P. J. Med. Chem. (2002) 45:5492–5505.
  • PIKE AC, BRZOZOWSKI AM, HUBBARD RE et al: Structure of the ligand-binding domain of estrogen receptor beta in the presence of a partial agonist and a full antagonist. EMBO J. (1999) 18:4608–4618.
  • MEYERS MJ, SUN J, CARLSON KE, KATZENELLENBOGEN BS, KATZENELLENBOGEN JA: Estrogen receptor subtype-selective ligands: asymmetric synthesis and biological evaluation of cis- and trans-5,11-dialky1-5,6,11,12-tetrahydrochrysenes. J. Med. Chem. (1999) 42:2456–2468.
  • GAUTHIER S, CARON B, CLOUTIER J et al: (5) (+) 4 [7 (2,2 Dimethy1-1-oxopropoxy)-4-methyl 2 [4 [2 (1 piperidiny1)-ethoxy]pheny11-2H-1-benzopyran-3-y11-phenyl 2,2-dimethylpropanoate (EM-800): a highly potent, specific, and orally active non-steroidal antiestrogen. Med. Chem. (1997) 40:2117–2122.
  • VAN DEVELDE P, NIQUE F, BOUCHOUX F et al.: RU-58668, a new pure antiestrogen inducing a regression of human mammary carcinoma implanted in nude mice. J. Steroid Biochem. Mol Biol. (1994) 48:187–196.
  • WATANABE N, IKENO A, MINATO H, NAKAGAWA H, KOHAYAKAWA C, TSUJI J: Discovery and preclinical characterization of (+) 3 [4 (1 piperidinoethoxy)phenyl]spiro rindene-1,1'-indane1-5,5'-diol hydrochloride: a promising non-steroidal estrogen receptor for hot flush. J. Med. Chem. (2003) 46:3961–3964.
  • KOBAYASHI T, TAMURA M, HAYASHI M et al.: Elevation of tail skin temperature in ovariectomized rats in relation to menopausal hot flushes. Am. J. Physiol: Regal, Integr: Comp. Physiol (2000) 278:R863–R869.
  • HOSONO T, CHEN X-M, MIYATSUJI Aet al.: Effects of estrogen on thermoregulatory tail vasomotion and heat-escape behavior in freely moving female rats. Am. J. Physiol: Regal, Integr. Comp. Physiol (2001), 280:R1341–R1347.
  • BERENDSEN HHG, WEEKERS AHJ, KLOOSTERBOER HJ: Effect of tibolone and raloxifene on the tail temperature of oestrogen-deficient rats. Ent Pharmacol (2001) 419:47–54.
  • MERCHENTHALER I, FUNKHOUSER JM, CARVER JM, LUNDEEN SG, GHOSH K, WINNEKER RC: The effect of estrogens and antiestrogens in a rat model for hot flush. Maturitas (1998) 30:307–316.
  • FINK BE, MORTENSEN DS, STAUFFER SR, ARON ZD, KATZENELLENBOGEN JA: Novel structural templates for estrogen-receptor ligands and prospects for combinatorial synthesis of estrogens. Chem. Biol. (1999) 4:205–219.
  • SCHOPFER U, SCHOEFFTER P, BISCHOFF SF, NOZULAK J, FEUERBACH D et al.: Toward selective ERI3 agonists for the central nervous system disorders: synthesis and characterization of aryl benzthiophenes. Med. Chem. (2002) 45:1399–1401.
  • MEYERS MJ, SUN J, CARLSON KE et al.: Estrogen receptor-I3 potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues. Med. Chem. (2001) 44:4230–4251.
  • MANAS ES: Design of compounds selective for the ERI3 receptor. IBC's 8th Annual World Congress Drug Discovery 7echnologyTM, Boston, USA (2003).
  • •Describes a presentation from Wyeth-Ayerst on their rationale and design of their ERP-selective compound, WAY-358.
  • JACQUOT Y, BERMONT L, GIORGI H et al.: Substituted benzopyranobenzothiazinones. Synthesis and estrogenic activity on MCF-7 breast carcinoma cells. Eui: Med. Chem. (2001) 36:127–136.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.