How were the 9,10-dihydrophenanthrene derivatives synthesized and tested for their inhibitory activity?

Label:chem

Topic
The study aimed to identify potent non-covalent inhibitors of SARS-CoV-2 3CLpro using a fluorescence resonance energy transfer (FRET) biochemical assay. The researchers synthesized a series of 9,10-dihydrophenanthrene derivatives and investigated their structure-activity relationships (SAR).
Answer
The 9,10-dihydrophenanthrene derivatives were synthesized using a rhodium (III)-catalyzed C-H activation and relay Diels-Alder reaction. The compounds were tested for their inhibitory activity against SARS-CoV-2 3CLpro using a FRET assay. The most potent compounds, C1 and C2, were further evaluated for their inhibitory mechanisms and metabolic stability.
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