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Total Synthesis of Bioactive Marine Meroterpenoids: The Cases of Liphagal and Frondosin B

1, 1 and 1,2,*
Key Laboratory of Marine Drugs, Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, 5 Yushan Road, Qingdao 266003, China
Laboratory for Marine Drugs and Bioproducts of Qingdao, National Laboratory for Marine Science and Technology (QNLM), 1 Wenhai Road, Qingdao 266237, China
Author to whom correspondence should be addressed.
Mar. Drugs 2018, 16(4), 115;
Received: 22 February 2018 / Revised: 28 March 2018 / Accepted: 28 March 2018 / Published: 31 March 2018
PDF [5603 KB, uploaded 31 March 2018]


Liphagal and frondosin B are two marine-derived secondary metabolites sharing a very similar polyfused-benzofuran skeleton. The two tetracyclic meroterpenoids were isolated from marine sponges, both featuring a 6-5-7-6 fused ring system. A preliminary bioactive study shows that (+)-liphagal is a selective kinase (PI3K α) inhibitor, while (+)-frondosin B is shown to inhibit the binding of the cytokine interleukin-8 (IL-8) to its receptor, CX-CLR1/2. The unique structures and interesting biological profiles of these two meroterpenoids have attracted considerable attention from synthetic chemists. Herein we summarize the synthetic efforts with respect to (+)-liphagal and (+)-frondosin B during the past two decades. View Full-Text
Keywords: natural product synthesis; total synthesis; liphagal; frondosin natural product synthesis; total synthesis; liphagal; frondosin

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Zong, Y.; Wang, W.; Xu, T. Total Synthesis of Bioactive Marine Meroterpenoids: The Cases of Liphagal and Frondosin B. Mar. Drugs 2018, 16, 115.

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