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Synthesis and biological evaluation of stilbene-based pure estrogen antagonists

Walter, Georg and Liebl, Renate and Angerer, Erwin von (2004) Synthesis and biological evaluation of stilbene-based pure estrogen antagonists. Bioorganic & Medicinal Chemistry Letters 14 (18), pp. 4659-4663.

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Abstract

Replacement of one of the ethyl substituents in diethylstilbestrol by side chains with functional groups converted this potent estrogen into pure antiestrogens with the potential for the treatment of breast cancer. These agents completely suppressed estrogen receptor-mediated gene activation and inhibited the growth of estrogen-sensitive MCF-7 breast cancer cells in submicromolar concentrations. ...

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Item Type:Article
Date:2004
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Identification Number:
ValueType
15324884PubMed ID
10.1016/j.bmcl.2004.06.098DOI
Classification:
NotationType
AnimalsMESH
Antineoplastic Agents/chemical synthesisMESH
Breast NeoplasmsMESH
Cell Line, TumorMESH
Estradiol/analogs & derivativesMESH
Estrogen Antagonists/chemical synthesisMESH
FemaleMESH
HumansMESH
MiceMESH
Organ Size/drug effectsMESH
Stilbenes/chemical synthesisMESH
Structure-Activity RelationshipMESH
Uterus/drug effectsMESH
Subjects:500 Science > 570 Life sciences
500 Science > 540 Chemistry & allied sciences
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Owner: Prof. Armin Buschauer
Deposited On:03 Dec 2008 15:58
Last Modified:05 Aug 2009 13:48
Item ID:4780
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