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ERa-selective agonists

A limited number of steroidal ERa-selective agonists have been described. [Pg.70]

Organon disclosed A510 steroids as ERa-selective agonists [50]. Compound 10 showed 290-fold ERa selectivity in a receptor-binding assay and over 50-fold ERa selectivity in a CHO cell-based transactivation assay. [Pg.71]

Indenoquinolines and Benzofluorenes Organon reported that indenoquinolines and benzofluorenes exhibit ERP-selective agonistic activity in CHO cells, stably transfected with ERP and ERa [98]. Attachment of a substituent at CIO was found... [Pg.85]

Estrogen agonists based on an oxabicyclic template [48] were described by Ligand. The enantiomers were separated and several of these compounds displayed potent affinity for the ERs. ER affinity and subtype selectivity was found to be dependent on the nature of the enantiomer and the presence of additional substituents. Thus, the ( +(-enantiomer 7 showed selectivity for ERa whereas the (—(-enantiomer 7 was selective for ERp. A further increase in binding affinity was observed for the 2, 2 -dimethyl analog 8. [Pg.70]

See other pages where ERa-selective agonists is mentioned: [Pg.86]    [Pg.50]    [Pg.66]    [Pg.68]    [Pg.69]    [Pg.110]    [Pg.116]    [Pg.368]    [Pg.86]    [Pg.50]    [Pg.66]    [Pg.68]    [Pg.69]    [Pg.110]    [Pg.116]    [Pg.368]    [Pg.151]    [Pg.414]    [Pg.152]    [Pg.59]    [Pg.66]    [Pg.70]    [Pg.110]    [Pg.264]    [Pg.237]    [Pg.754]    [Pg.1129]    [Pg.340]    [Pg.143]    [Pg.73]    [Pg.132]    [Pg.227]    [Pg.149]    [Pg.150]    [Pg.152]    [Pg.156]    [Pg.93]    [Pg.30]    [Pg.20]    [Pg.26]    [Pg.52]    [Pg.221]    [Pg.265]    [Pg.221]    [Pg.754]    [Pg.1129]    [Pg.40]    [Pg.39]    [Pg.35]    [Pg.54]    [Pg.68]    [Pg.72]    [Pg.76]    [Pg.88]   
See also in sourсe #XX -- [ Pg.51 , Pg.69 , Pg.88 , Pg.110 , Pg.115 ]



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