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Volumn 14, Issue 10, 2004, Pages 2551-2554

Estrogen receptor ligands. Part 3: The SAR of dihydrobenzoxathiin SERMs

Author keywords

Dihydrobenzoxathiin; SERAMs; SERMs

Indexed keywords

ANTIESTROGEN; DIHYDROBENZOXATHIIN; ESTROGEN RECEPTOR; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; LIGAND; RECEPTOR SUBUNIT; UNCLASSIFIED DRUG;

EID: 11144354858     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.02.084     Document Type: Article
Times cited : (46)

References (23)
  • 6
    • 0037435046 scopus 로고    scopus 로고
    • Recent reviews on SERMs:
    • Recent reviews on SERMs: Jordan V.C. J. Med. Chem. 46:2003;883.
    • (2003) J. Med. Chem. , vol.46 , pp. 883
    • Jordan, V.C.1
  • 16
    • 1942427981 scopus 로고    scopus 로고
    • U.S. Patent 2,276,553; 2,332,418
    • (b) The thiophenols 3 were prepared by known procedures with minor modifications: Werner, G.; Biebrich, W. U.S. Patent 2,276,553; 2,332,418
    • Werner, G.1    Biebrich, W.2
  • 18
    • 0029152136 scopus 로고
    • The lithium anions of 3- and 4-picoline were prepared according to previously reported method:
    • The lithium anions of 3- and 4-picoline were prepared according to previously reported method: Koller M.U., Peariso K.L., Guion T., Martinez S.S., Beam C.F. Synth. Commun. 25:1995;2963-2974.
    • (1995) Synth. Commun. , vol.25 , pp. 2963-2974
    • Koller, M.U.1    Peariso, K.L.2    Guion, T.3    Martinez, S.S.4    Beam, C.F.5
  • 21
    • 1942492269 scopus 로고    scopus 로고
    • note
    • 50 values were generated in an estrogen receptor ligand binding assay. This scintillation proximity assay was conducted in NEN Basic Flashplates using tritiated estradiol and full length recombinant human ERα and ERβ proteins with a 3 h incubation time. Most compounds are single point determinants unless otherwise indicated by standard deviation where n =2-5.
  • 22
    • 1942427977 scopus 로고    scopus 로고
    • note
    • ′-chloro)tricyclo[3.3.1.13,7] decan}-4-yl)phenyl phosphate] in white 96 well plates and product formation was measured using a microplate luminometer. An integral measurement with 1-s reading of each well was used. ALP activity was expressed in light units (LU), which was directly proportional to the level of ALP expression from the cells.
  • 23
    • 1942492268 scopus 로고    scopus 로고
    • note
    • Twenty-day old intact Sprague-Dawley rats were treated (sc) with test compounds for 3 days at 1 mpk. The anti-estrogenic activity of compounds was determined by co-administration of the compound with a subcutaneous injection of 17-β-estradiol and reported as % inhibition. The estrogenic activity (partial agonism) of the compounds was determined by administering the test compound without estradiol and reported as % control.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.