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3-Alkyl-2-phenylbenzo[b]thiophenes: nonsteroidal estrogen antagonists with mammary tumor inhibiting activity

Angerer, Erwin von and Erber, Sebastian (1992) 3-Alkyl-2-phenylbenzo[b]thiophenes: nonsteroidal estrogen antagonists with mammary tumor inhibiting activity. The Journal of steroid biochemistry and molecular biology 41 (3-8), pp. 557-562.

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Abstract

A number of 2-(4-hydroxyphenyl)benzo[b]thiophenes with a hydroxy group in position 5 or 6 and a short alkyl group at C-3 were synthesized and studied for their estrogen receptor affinities. Relative binding affinities (RBA) for the calf uterine estrogen receptor ranged from 3 to 60 (17 beta-estradiol = 100). The highest RBA values were found with ethyl derivatives [3 (5-OH): 60; 7 (6-OH): 28]. In ...

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Item Type:Article
Date:1992
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Projects:SFB 234
Identification Number:
ValueType
1562527PubMed ID
Classification:
NotationType
AnimalsMESH
Antineoplastic Agents/chemical synthesisMESH
Breast NeoplasmsMESH
Cell Division/drug effectsMESH
Cell Survival/drug effectsMESH
Drug Screening Assays, AntitumorMESH
Estrogen Antagonists/chemical synthesisMESH
FemaleMESH
HumansMESH
Indicators and ReagentsMESH
Mammary Neoplasms, Experimental/drug therapyMESH
MiceMESH
Mice, Inbred StrainsMESH
Molecular StructureMESH
Organ Size/drug effectsMESH
Receptors, Estradiol/drug effectsMESH
Structure-Activity RelationshipMESH
Thiophenes/chemical synthesisMESH
Uterus/anatomy & histologyMESH
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 14:37
Last Modified:05 Aug 2009 13:48
Item ID:4756
Owner Only: item control page
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