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Synthesis and properties of some new 3-substituted hexestrol derivatives

par Vilkas, Michel;Masamba, Luzolo;Makani, Siku;Leclercq, Guy
Référence European journal of medicinal chemistry, 22, 1, page (27-31)
Publication Publié, 1987

Article révisé par les pairs

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Résumé :

A series of new monosubstituted hexestrol derivatives were synthesized and the estrogenic and cytotoxic properties of some of them were studied. 3-Acetoxymethyl-hexestrol 8 has a binding affinity for the cytoplasmic estrogen receptor as high as estradiol. It is 100-1000 times lower for the coumarinic derivatives 13, 14 and 15. None of these compounds becomes covalently bound to the receptor. They display a 20-1000 times lower affinity for the estrogen receptor in the whole cell test on the MCF-7 mammary tumor cell culture. At low concentrations (10-8 M) the three coumarinic derivatives stimulate the growth of these cells (estrogenic effect) as strongly as estradiol does. © 1987.