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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
10
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pubmed:dateCreated |
1982-4-20
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pubmed:abstractText |
The syntheses of the meso-1,2-dialkyl-1,2-bis(3'-hydroxyphenyl)ethanes [alkyl substituent: CH3 (19), C2H5 (20), C3H7 (22), C4H9 (23), i-C4H9 (24), and C5H11 (25)] and of d,l-3,4-bis(3'-hydroxyphenyl)hexane (21) are described. In vitro these compounds inhibited the [3H]estradiol receptor interaction competitively, exhibiting Ka values between 0.20 x 10(9) (20) and 0.11 x 10(6) M-1 (24). In vivo the meso compounds reduced the estrone-stimulated mouse uterine growth; the most effective compounds were 20, 22, and 23 (53, 50, and 45% inhibition, respectively). Compounds 20 and 22-24 showed weak estrogenic activity in the mouse uterine weight test and in the vaginal cornification test. Compounds 19 (NSC-297169), 20 (NSC-297170), and 22 (NSC-297171) exhibited a dose-dependent growth inhibition on the MCF-7 human breast tumor cell line (10(-6) to 10(-9) M). These compounds also showed a marked dose-dependent inhibition on the DMBA-induced, hormone-dependent mammary carcinoma of the Sprague-Dawley rat corresponding to their association constants.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
24
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1192-7
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:6276542-Animals,
pubmed-meshheading:6276542-Antineoplastic Agents,
pubmed-meshheading:6276542-Cell Line,
pubmed-meshheading:6276542-Dose-Response Relationship, Drug,
pubmed-meshheading:6276542-Estrogen Antagonists,
pubmed-meshheading:6276542-Female,
pubmed-meshheading:6276542-Hexestrol,
pubmed-meshheading:6276542-Humans,
pubmed-meshheading:6276542-Mammary Neoplasms, Experimental,
pubmed-meshheading:6276542-Mice,
pubmed-meshheading:6276542-Mice, Inbred Strains,
pubmed-meshheading:6276542-Rats,
pubmed-meshheading:6276542-Rats, Inbred Strains,
pubmed-meshheading:6276542-Uterus
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pubmed:year |
1981
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pubmed:articleTitle |
Potential antiestrogens. Synthesis and evaluation of mammary tumor inhibiting activity of 1,2-dialkyl-1,2-bis(3'-hydroxyphenyl)ethanes.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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