Antitumor agents. 266. Design, synthesis, and biological evaluation of novel 2-(furan-2-yl)naphthalen-1-ol derivatives as potent and selective antibreast cancer agents.

Antitumor agents. 266. Design, synthesis, and biological evaluation of novel 2-(furan-2-yl)naphthalen-1-ol derivatives as potent and selective antibreast cancer agents.
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DOI:
10.1021/jm9001567
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发表时间:
2009-06-11
影响因子:
7.3
通讯作者:
Lee KH
Lee KH
中科院分区:
医学1区
文献类型:
--
作者:
Dong Y;Shi Q;Liu YN;Wang X;Bastow KF;Lee KH

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在一项持续的研究中,我们探索了新丹参内酯(1)中的单个环如何影响其有效和选择性的体外抗乳腺癌活性。因此,我们发现了一类新的抗乳腺癌药物,2-(呋喃-2-基)萘-1-醇衍生物,基于活性C-环开放的模型化合物5。进一步优化得到18和21,其显示出降低的细胞毒性效力,但比新丹参内酯类似物2具有更好的选择性。有趣的是,化合物20对人癌细胞系显示出广泛的细胞毒性。
In a continuing study, we explored how the individual rings in neo-tanshinlactone (1) influence its potent and selective in vitro anti-breast cancer activity. Accordingly, we discovered a novel class of anti-breast cancer agents, 2-(furan-2-yl) naphthalen-1-ol derivatives, based on an active C-ring opened model compound 5. Further optimization led to 18 and 21, which showed decreased cytotoxic potency, but better selectivity than neo-tanshinlactone analog 2. Interestingly, compound 20 showed broad cytotoxicity against human cancer cell lines.
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