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Synthesis and biological properties of a 1-(6-aziridinylhexyl)-2-phenylindole, a potential fluorescence label for estrogen receptors

Erber, S. and Birnböck, H. and Angerer, E. von (1990) Synthesis and biological properties of a 1-(6-aziridinylhexyl)-2-phenylindole, a potential fluorescence label for estrogen receptors. Archiv der Pharmazie 323 (8), pp. 459-463.

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Abstract

2-Phenylindole derivative 8, linked to aziridine by a hexamethylene spacer group, was synthesized and tested. It binds to the estrogen receptor with an RBA-value of 4.0 (estradiol = 100). In vitro, it shows a selective cytostatic activity in hormone-dependent MCF-7 breast cancer cells (41% T/C at 10(-6) M). In vivo, it exerts a strong estrogenic effect. The binding to the estrogen receptor is ...

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Item Type:Article
Date:1990
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Projects:SFB 234
Identification Number:
ValueType
2278511PubMed ID
Classification:
NotationType
AnimalsMESH
Aziridines/chemical synthesisMESH
Breast Neoplasms/pathologyMESH
ChemistryMESH
FemaleMESH
Fluorescent Dyes/chemical synthesisMESH
HumansMESH
Indoles/chemical synthesisMESH
MiceMESH
Receptors, Estrogen/drug effectsMESH
Tumor Cells, Cultured/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:10 Dec 2008 16:08
Last Modified:05 Aug 2009 13:48
Item ID:4741
Owner Only: item control page
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