Construction of Benzofuranone Library via Metal-Free, One-Pot Intermolecular Condensation and Their Application as Efficient Estrogen Receptor β Modulators

Facile synthesis of benzofuranone was achieved through a metal-free, one-pot, intermolecular condensation between -hydroxy aryl ketones and resorcinol derivatives. A library of 20 compounds was prepared with moderate to good overall yields. These compounds showed strong binding toward estrogen receptors along with good selectivity for ERβ (>190-fold over ERα). Anti-proliferative activity on DU-145, U-87, and MCF-7 cells gave inhibition IC50 in the low uM range, which suggested the promising potential therapeutic applications of these new class of benzofuranones.