Selective estrogen receptor modulators (SERMs) are a class of drugs that act on the estrogen receptor (ER). SERMs are used for treatment and reduction of risk of breast cancer. Herewith we had designed, synthesized and evaluated chalcone-phenylpyran-2-one derivatives bearing N,N-dimethyl ethalamine side chain for their anti-breast cancer activity using MCF-7 and Zr-75-1 cell lines in-vitro. The pharmacological data indicated that most of tested compounds showed moderate to significant cytotoxicity and high selectivity toward estrogen receptor. The SAR analyses indicated that compounds 5f with 2,6 dichloro substitution was more effective. Docking study was performed to predict binding orientation towards the estrogen receptor-α.
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Retraction: Cirujano, F. Ionic liquids vs. Microporous Solids as Reusable Reaction Media for the Catalytic C–H Functionalization of Indoles with Alcohols. In Proceedings of the 22nd International Electronic Conference on Synthetic Organic Chemistry, 15 November–15 December 2019; Sciforum Electronic Conference Series, doi: 10.3390/ecsoc-22-05655
Design and Synthesis of Novel chalcone-phenylpyranone derivatives as Estrogen Receptor Modulators
Published: 23 November 2018 by MDPI in The 22nd International Electronic Conference on Synthetic Organic Chemistry session Bioorganic, Medicinal and Natural Products Chemistry
Keywords: SERM, breast cancer, chalcone, phenylpyranone, MCF-7, Docking