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

被引：57

作者：

Lin, An-Shen

Nakagawa-Goto, Kyoko

Chang, Fang-Rong

Yu, Donglei

Morris-Natschke, Susan L.

Wu, Chin-Chung

Chen, Shu-Li

Wu, Yang-Chang ^{[1
]}

Lee, Kuo-Hsiung

机构：

[1] Natl Sun Yat Sen Univ, Kaohsiung Med Univ Joint Res Ctr, Kaohsiung 80424, Taiwan

[2] Univ N Carolina, Sch Pharm, Nat Prod Res Labs, Chapel Hill, NC 27599 USA

[3] Kaohsiung Med Univ, Grad Inst Nat Prod, Kaohsiung 807, Taiwan

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2007年 / 50卷 / 16期

关键词：

D O I：

10.1021/jm070363a

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 I 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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页码：3921 / 3927

页数：7

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