Pharmacological profile of 6, 12-dihydro-3-methoxy-1-benzopyrano [3, 4-b][1, 4] benzothiazin-6-one, a novel human estrogen receptor agonist.

…, Y Ma, A Boulahdour, L Bermont, B Refouvelet…

Index: Jacquot, Yves; Cleeren, Anny; Laios, Ioanna; Ma, Yan; Boulahdour, Athem; Bermont, Laurent; Refouvelet, Bernard; Adessi, Gerard; Leclercq, Guy; Xicluna, Alain Biological and Pharmaceutical Bulletin, 2002 , vol. 25, # 3 p. 335 - 341

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Citation Number: 12

Abstract

Pharmacological studies were carried out to characterize further the endocrinological profile and the binding mode to the estrogen receptor (ER) of 6, 12-dihydro-3-methoxy-1- benzopyrano [3, 4-b][1, 4] benzothiazin-6-one (1). Binding experiments were conducted with highly purified recombinant human estrogen receptors hERα and β. Potent estrogenic activity of compound 1 was assessed by testing its ability to down-regulate ERs and to ...