Antiestrogenic hydrazones

Details Antiestrogenic hydrazones Antiestrogenic hydrazones

C - Chemistry, Metallurgy

07

C

167/228, 167/273

C07C 251/74 (2006.01) A61K 31/15 (2006.01) C07D 213/53 (2006.01) C07D 213/65 (2006.01)

Patent

CA 1331460

ANTIESTROGENIC HYDRAZONES ABSTRACT Azido-, 4-nitro and 2,4-dinitrophenylhydrazones as well as 4,4'-dihydroxybenzophenone-hydrazone 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-dinitrophenyl 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.

541063

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