2. Academic Validation
  3. First total synthesis of protoapigenone and its analogues as potent cytotoxic agents

First total synthesis of protoapigenone and its analogues as potent cytotoxic agents

  • J Med Chem. 2007 Aug 9;50(16):3921-7. doi: 10.1021/jm070363a.
An-Shen Lin 1,  Kyoko Nakagawa-Goto,  Fang-Rong Chang,  Donglei Yu,  Susan L Morris-Natschke,  Chin-Chung Wu,  Shu-Li Chen,  Yang-Chang Wu,  Kuo-Hsiung Lee
Affiliations

Affiliation

  • 1 Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung 807, Taiwan.
PMID: 17622129 DOI: 10.1021/jm070363a
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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