The inhibitory effect of 5-acetoxy-2-(4-acetoxyphenyl)-1-ethyl-3-methylindole (D 16726) on estrogen-dependent mammary tumors
| Autor: | Martin R. Berger, J. Prekajac, Erwin von Angerer |
|---|---|
| Rok vydání: | 1985 |
| Předmět: |
medicine.medical_specialty
Indoles Neoplasms Hormone-Dependent medicine.drug_class 9 10-Dimethyl-1 2-benzanthracene Mammary gland Estrogen receptor Breast Neoplasms Mice Inbred Strains Mice In vivo Internal medicine medicine Animals Humans skin and connective tissue diseases Mode of action Mammary tumor Chemistry Mammary Neoplasms Experimental Methylnitrosourea Rats Inbred Strains Antiestrogen Rats Tamoxifen medicine.anatomical_structure Endocrinology Oncology Mechanism of action Receptors Estrogen Estrogen Female medicine.symptom Neoplasm Transplantation |
| Zdroj: | European journal of cancerclinical oncology. 21(4) |
| ISSN: | 0277-5379 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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