Miscellaneous ERP Ligands

Natural Products Bionovo reported phase II clinical development of MF-101, an ERp agonist, for the treatment of vasomotor symptoms in pre- and postmenopausal women. Two doses (5 and 10g) of MF-101 were more effective than placebo at reducing the frequency and severity of hot flashes. MF-101 is an aqueous ethanol extract of 22 herb species and showed selective ERp recruitment to target genes [105], 

Bicyclononene Ring Systems Bayer disclosed ERligands that are derived from a rigid bicyclo-[3.3.1]-nonene core [106]. This series was derived from the prototype bicyclic ether 89a, which was identified by HTS. This type of scaffold is unusual in the field of estrogen templates reported thus far. Improved ERp affinity and ERp selectivity was observed for the bicyclo-[3.3.1]-nonene derivative 89b. However, compound 89b was tested as an enantiomeric mixture making it difficult to draw conclusions on further prospects of this series. 

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