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Synthesis via atroposelective Mizoroki-Heck reaction shows potent antiproliferation in breast cancer cells.
(-)-Steganacin is a lignan with a unique dibenzocyclooctadiene lactone framework. Herein, we describe the total synthesis of (-)-steganacin and its congeners through a stereocontrolled atroposelective intramolecular Mizoroki-Heck reaction. The synthesis of (-)-steganacin was completed in 11 steps from commercial substrates with a 7% overall yield. Furthermore, the biological activities of (-)-steganacin and its synthetic analogues were evaluated. (-)-Steganacin exhibits potent antiproliferation activity against MDA-MB-468 breast cancer cells with IC50 = 0.50 μM.
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Yang et al. (2025) studied this question.
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