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2-Phenylindoles. Effect of N-benzylation on estrogen receptor affinity, estrogenic properties, and mammary tumor inhibiting activity

Angerer, E. von and Strohmeier, J. (1987) 2-Phenylindoles. Effect of N-benzylation on estrogen receptor affinity, estrogenic properties, and mammary tumor inhibiting activity. Journal of medicinal chemistry 30 (1), pp. 131-136.

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Abstract

Hydroxy-2-phenylindoles carrying substituted benzyl groups and similar substituents at the nitrogen were synthesized and tested for their ability to displace estradiol from its receptor. All of the derivatives tested exhibited high binding affinities for the calf uterine estrogen receptor, with RBA values ranging from 0.55 to 16 (estradiol 100). The mouse uterine weight tested revealed only low ...

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Item Type:Article
Date:1987
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Projects:SFB 234
Identification Number:
ValueType
3806590PubMed ID
Classification:
NotationType
AnimalsMESH
Antineoplastic Agents/chemical synthesisMESH
Breast Neoplasms/pathologyMESH
CattleMESH
Cell Division/drug effectsMESH
Cell LineMESH
Drug Evaluation, PreclinicalMESH
Estrogen Antagonists/chemical synthesisMESH
FemaleMESH
HumansMESH
Indicators and ReagentsMESH
Indoles/chemical synthesisMESH
Mammary Neoplasms, Experimental/drug therapyMESH
RatsMESH
Rats, Inbred StrainsMESH
Receptors, Estrogen/drug effectsMESH
Structure-Activity RelationshipMESH
Uterus/metabolismMESH
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 14:46
Last Modified:05 Aug 2009 13:48
Item ID:4735
Owner Only: item control page
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