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Updated: Sep 17, 2025

A High-Throughput Luciferase Assay to Evaluate Proteolysis of the Single-Turnover Protease PCSK9
Published on: August 28, 2018
Collective Synthesis and PCSK9 Inhibitory Activities of Pavine and Isopavine Alkaloids
Xiaohui Geng1, Cunyu Feng1, Xuan Pan1
1State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, P. R. China.
Abstract:
An efficient approach for the synthesis of pavine and isopavine alkaloids through photoredox-catalyzed intramolecular cyclization is disclosed, which features low catalyst dosage and good functional group compatibility. A total of 18 natural products, including 10 pavine and 8 isopavine alkaloids as well as 20 analogs, have been successfully synthesized by this protocol. A plausible reaction mechanism was also proposed. Moreover, preliminary PCSK9 inhibitory activities of these compounds were evaluated. Compound 1'f exhibited the most potent PCSK9 inhibitory activity with the IC50 value of 161 nM, superior to the positive control berberine.
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