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

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.

• Authors: E von Angerer, J Prekajac, M Berger
• Journal: European journal of cancer & clinical oncology (Eur J Cancer Clin Oncol) Vol. 21 Issue 4 Pg. 531-7 (Apr 1985) ISSN: 0277-5379 [Print] England
• PMID: 3924626 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Indoles
• Receptors, Estrogen
• Tamoxifen
• zindoxifene
• 9,10-Dimethyl-1,2-benzanthracene
• Methylnitrosourea

Topics

• 9,10-Dimethyl-1,2-benzanthracene
• Animals
• Breast Neoplasms (pathology)
• Female
• Humans
• Indoles (therapeutic use)
• Mammary Neoplasms, Experimental (chemically induced, drug therapy)
• Methylnitrosourea
• Mice
• Mice, Inbred Strains
• Neoplasm Transplantation
• Neoplasms, Hormone-Dependent (drug therapy)
• Rats
• Rats, Inbred Strains
• Receptors, Estrogen (metabolism)
• Tamoxifen (therapeutic use)