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Construction of benzofuranone library via a metal-free, one-pot intermolecular condensation, and their application as efficient estrogen receptor β modulators

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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.

Graphical abstract: Construction of benzofuranone library via a metal-free, one-pot intermolecular condensation, and their application as efficient estrogen receptor β modulators

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Publication details

The article was received on 25 Jul 2019, accepted on 02 Oct 2019 and first published on 02 Oct 2019


Article type: Communication
DOI: 10.1039/C9CC05756K
Chem. Commun., 2019, Advance Article

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    Construction of benzofuranone library via a metal-free, one-pot intermolecular condensation, and their application as efficient estrogen receptor β modulators

    X. Peng, Z. Hu, J. Zhang, W. Ning, S. Zhang, C. Dong, X. Shi and H. Zhou, Chem. Commun., 2019, Advance Article , DOI: 10.1039/C9CC05756K

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