Synthesis, structure, and biological properties of some 8alpha-analogues of steroid estrogens with fluorine in position 2

A total synthesis of 8alpha analogues of steroid estrogens with fluorine in position 2 was achieved. Structural features of these compounds were studied by the example of 17beta-acetoxy-2-fluoro-3-methoxy-8alpha-estra-1,3,5(10)-triene. It was shown that the 8alpha analogues of 2-fluorosubstituted st...

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Bibliographic Details
Published in:	Bioorganicheskaia khimiia Vol. 33; no. 3; p. 315
Main Authors:	Belov, V N, Dudkin, V Iu, Urusova, E A, Starova, G L, Selivanov, S I, Nikolaev, S V, Eshchenko, N D, Morozkina, S N, Shavva, A G
Format:	Journal Article
Language:	Russian
Published:	Russia (Federation) 01-05-2007
Subjects:	Animals Anticholesteremic Agents - chemical synthesis Anticholesteremic Agents - chemistry Anticholesteremic Agents - pharmacology Bone Density - drug effects Bone Density Conservation Agents - chemical synthesis Bone Density Conservation Agents - chemistry Bone Density Conservation Agents - pharmacology Cholesterol - blood Estrenes - chemical synthesis Estrenes - chemistry Estrenes - pharmacology Estrogens - chemical synthesis Estrogens - chemistry Estrogens - pharmacology Female Fluorine Rats Rats, Sprague-Dawley Structure-Activity Relationship Uterus - drug effects
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Summary:	A total synthesis of 8alpha analogues of steroid estrogens with fluorine in position 2 was achieved. Structural features of these compounds were studied by the example of 17beta-acetoxy-2-fluoro-3-methoxy-8alpha-estra-1,3,5(10)-triene. It was shown that the 8alpha analogues of 2-fluorosubstituted steroid estrogens have a low uterotropic activity and retain the osteoprotective and hypocholesterolemic activities.
ISSN:	0132-3423