Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1985-09-16
1988-03-22
Jiles, Henry R.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514351, 514639, 514874, 546300, 546332, 260349, 564251, C07D21353, C07D21365, C07C10914, A61K 3144
Patent
active
047329041
ABSTRACT:
Azido-, 4-nitro and 2,4-dinitrophenylhydrazones as well as 4,4'-dihydroxybenzophenone-hydrazone and other hydrazones are disclosed which have antiestrogenic activity useful in treating estrogen-requiring tumor cells. The described hydrazones bind to estrogen receptors in the cytoplasm of tumor cells. The azido-, 4-nitro- and 2,4-dinitro-phenyl branches of the molecules appear to bind to the receptors and prevent translocation of estrogenic information into the nucleus, thereby blocking the synthesis of necessary macromolecules such as proteins. Absence of geometric isomerization from antiestrogenic to estrogenic forms of the drug minimizes estrogenic side-effects.
REFERENCES:
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Chemical Abstracts 94:8153p (Soria et al).
Shriner, R. L. et al, "Systematic Identification of Organic Compounds", 4th edition (1956), pp. 214-219, 316-319.
Chemical Abstracts 73:14634d (LeGoff et al.).
Chemical Abstracts 77:60926f (Brown et al).
Chemical Abstracts 89:110153x (Olsson et al).
Bjorkman Dale A.
Jiles Henry R.
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