Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 7, Issue 1, Pages 94-99Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.5b00413
Keywords
Estrogen receptor; antagonist; downregulator; bioavailable; phenol; tetrahydroisoquinoline
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A series of tetrahydroisoquinoline phenols was modified to give an estrogen receptor downregulator-antagonist profile. Optimization around the core, alkyl side chain, and pendant aryl ring resulted in compounds with subnanomolar levels of potency. The phenol functionality was shown to be required to achieve highly potent compounds, but unusually this was compatible with obtaining high oral bioavailabilities in rat.
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