2001 thiazine derivatives

thiazine derivativesR 0610

35 - 168Substituted Benzopyranobenzothiazinones. Synthesis and EstrogenicActivity on MCF-7 Breast Carcinoma Cells. — Six compounds oftype (III) and (IV) are prepared and their estrogenic effect is evaluated onthe proliferation of MCF-7 breast adenocarcinoma cells. Compounds (IIIc)and (IV) exhibit an estrogen receptor-dependent proliferation and a highbinding affinity to estrogen receptors, but a moderate capacity to activate thetranscription of a reporter gene. Their pharmacological profiles are definedby their binding properties and their mechanism of action by computationalmodeling studies. — (JACQUOT, YVES; BERMONT, LAURENT; GIORGI,HERVE; REFOUVELET, BERNARD; ADESSI, GERARD L.; DAUBROSSE,EDWIGE; XICLUNA, ALAIN; Eur. J. Med. Chem. 36 (2001) 2, 127-136;Equipe Chim. Ther., Fac. Med. Pharm., Univ. Franche-Comte, F-25030Besancon, Fr.; EN)

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