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Total Synthesis and Biological Evaluation of Phaeosphaerides

Graduate School of Pharmaceutical Sciences, Meiji Pharmaceutical University, 2-522-1 Noshio, Kiyose, Tokyo 204-8588, Japan
Author to whom correspondence should be addressed.
Catalysts 2018, 8(5), 206;
Received: 26 April 2018 / Revised: 5 May 2018 / Accepted: 7 May 2018 / Published: 14 May 2018
(This article belongs to the Special Issue Catalyzed Synthesis of Natural Products)
PDF [2290 KB, uploaded 14 May 2018]


This article reviews studies regarding the total synthesis of phaeosphaerides A and B, nitrogen-containing bicyclic natural products isolated from an endophytic fungus. Numerous synthetic efforts and an X-ray crystal structure analysis of phaeosphaeride A have enabled revision of its originally proposed structure. In addition, a successful protic acid-mediated transformation of phaeosphaeride A to phaeosphaeride B revealed the hypothetical biosynthesis of phaeosphaeride B from phaeosphaeride A. Structure–activity relationship studies of phaeosphaeride derivatives are also discussed. View Full-Text
Keywords: phaeosphaeride A; phaeosphaeride B; total synthesis; structural revision; STAT3; anticancer phaeosphaeride A; phaeosphaeride B; total synthesis; structural revision; STAT3; anticancer

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Kobayashi, K.; Tanaka, K., III; Kogen, H. Total Synthesis and Biological Evaluation of Phaeosphaerides. Catalysts 2018, 8, 206.

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