Construction of benzofuranone library via a metal-free, one-pot intermolecular condensation, and their application as
Xueke Peng1, Zhiye Hu1, Jing Zhang1
1State Key Laboratory of Virology, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (Wuhan University), Ministry of Education, Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, Wuhan University School of Pharmaceutical Sciences, Wuhan 430071, China. zhouhb@whu.edu.cn.
Abstract:
Facile synthesis of benzofuranone was achieved through a metal-free, one-pot intermolecular condensation between α-hydroxy aryl ketones and resorcinol derivatives. A library of 20 compounds with moderate to good overall yields was prepared. 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 values in the low μM range, which suggested the promising potential therapeutic applications of these new classes of benzofuranones.
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