2-(Hydroxyphenyl)indoles: a new class of mammary tumor-inhibiting compounds
| Autor: | Erwin von Angerer, J. Prekajac |
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| Rok vydání: | 1983 |
| Předmět: |
Indoles
Chemical Phenomena Stereochemistry 9 10-Dimethyl-1 2-benzanthracene DMBA Estrogen receptor Antineoplastic Agents Mammary carcinoma chemistry.chemical_compound Mice Estradiol Congeners Drug Discovery Animals Humans Ether cleavage Alkyl Cells Cultured chemistry.chemical_classification Dansyl Compounds Anthracene Mammary tumor Uterus Dual mode Estrogen Antagonists Mammary Neoplasms Experimental Rats Inbred Strains Molecular biology Rats Chemistry Methotrexate chemistry 540 Chemie Molecular Medicine Cattle Female |
| DOI: | 10.5283/epub.14972 |
| Popis: | 1-Alkyl-4-chloro-2-(2,6-dichloro-4-hydroxyphenyl)-6-hydroxyindoles (4, alkyl = CH3, C2H5, C3H7) were synthesized by thermolysis of the corresponding N,N'-dialkyl-1,2-diphenylethylenediamines and subsequent ether cleavage. They showed an affinity for the estrogen receptor (1% of 17 beta-estradiol) and inhibited the growth of the 9,10-dimethyl-1,2-benz[a]anthracene (DMBA) induced mammary carcinoma of the Sprague-Dawley (SD) rat. The best result was obtained by the ethyl compound (4b), which reduced the original tumor area by 50% after 4 weeks administration of 6 X 18 (mg/kg)/week. Since 4a and 4b show uterotrophic activity and cytostatic effects against hormone-independent cells, a dual mode of action has to be considered for the tumor inhibition. |
| Databáze: | OpenAIRE |
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