The inhibitory effect of 5-acetoxy-2-(4-acetoxyphenyl)-1-ethyl-3-methylindole (D 16726) on estrogen-dependent mammary tumors

Angerer, E. von ; Prekajac, J. ; Berger, M.

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Details

Item type:	Article
Journal or Publication Title:	European journal of cancer & clinical oncology
Volume:	21
Number of Issue or Book Chapter:	4
Page Range:	pp. 531-537
Date:	1985
Institutions:	Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Projects:	DFG Projekt An 139/1
Identification Number:	Value Type 3924626 PubMed ID
Classification:	Notation Type 9,10-Dimethyl-1,2-benzanthracene MESH Animals MESH Breast Neoplasms/pathology MESH Female MESH Humans MESH Indoles/therapeutic use MESH Mammary Neoplasms, Experimental/chemically induced MESH Methylnitrosourea MESH Mice MESH Mice, Inbred Strains MESH Neoplasm Transplantation MESH Neoplasms, Hormone-Dependent/drug therapy MESH Rats MESH Rats, Inbred Strains MESH Receptors, Estrogen/metabolism MESH Tamoxifen/therapeutic use MESH
Dewey Decimal Classification:	500 Science > 570 Life sciences 500 Science > 540 Chemistry & allied sciences 600 Technology > 610 Medical sciences Medicine
Status:	Published
Refereed:	Yes, this version has been refereed
Created at the University of Regensburg:	Yes
Item ID:	4728

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Abstract

The antineoplastic activity of the antiestrogen 5-acetoxy-2-(4-acetoxyphenyl)-1-ethyl-3-methylindole (D 16726) was determined in several estrogen-dependent mammary tumor models. The growth of the DMBA-induced rat mammary carcinoma was inhibited by doses ranging from 1 to 12 mg/kg. The maximum decrease of tumor area was 67% (control + 635%). D 16726 was also active against MNU-induced rat mammary ...

Abstract

The antineoplastic activity of the antiestrogen 5-acetoxy-2-(4-acetoxyphenyl)-1-ethyl-3-methylindole (D 16726) was determined in several estrogen-dependent mammary tumor models. The growth of the DMBA-induced rat mammary carcinoma was inhibited by doses ranging from 1 to 12 mg/kg. The maximum decrease of tumor area was 67% (control + 635%). D 16726 was also active against MNU-induced rat mammary tumors and transplanted MXT tumors of the mouse. The growth of estrogen receptor-positive MCF-7 breast cancer cells was inhibited by the hydroxy derivative D 15414 (10(-8)-10(-5) M). Because of the high binding affinity of D 15414 for the estrogen receptor (RBA 6.7-10.0) and the lack of activity against hormone-independent MDA-MB 231 breast cancer cells, a specific mode of action involving the estrogen receptor is likely.

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