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  • Title: First total synthesis of protoapigenone and its analogues as potent cytotoxic agents.
    Author: Lin AS, Nakagawa-Goto K, Chang FR, Yu D, Morris-Natschke SL, Wu CC, Chen SL, Wu YC, Lee KH.
    Journal: J Med Chem; 2007 Aug 09; 50(16):3921-7. PubMed ID: 17622129.
    Abstract:
    Protoapigenone (1), isolated from Thelypteris torresiana, previously showed significant cytotoxic activity against five human cancer cell lines. In a continued structure-activity relationship study, the first total synthesis and modification of 1 were achieved. All synthesized compounds and related intermediates were evaluated for cytotoxic activity against five human cancer cell lines, HepG2, Hep3B, MDA-MB-231, MCF-7, and A549. Among them, 24 showed 2.2-14.2-fold greater cytotoxicity than 1 and naphthyl A-ring analogues remarkably enhanced the activity.
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