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学科主题: 天然产物有机化学
题名: Design, synthesis, and biological evaluation of novel trifluoromethyl indoles as potent HIV-1 NNRTIs with an improved drug resistance profile
其他题名: 新型三氟甲基吲哚类HIV-1 NNRTIs的设计、合成及活性研究
作者: Jiang HX(姜海霞)1; Zhuang DM(庄道明)1; Huang Y(黄迎)1; Cao XX(曹欣欣)1; Yao JH(姚建华)1; Li JY(李敬云)1; Wang JY(王建永)1; Zhang C(张琛)1; Jiang B(姜标)1
通讯作者: 张琛 ; 姜标
刊名: Org. Biomol. Chem.
发表日期: 2014
DOI: 10.1039/c3ob42186d
卷: 12, 期:21, 页:3446-3458
收录类别: SCI
英文摘要: novel series of trifluoromethyl indole derivatives have been designed, synthesized and evaluated for anti-HIV-1 activities in MT-2 cells. The hydrophobic constant, acute toxicity, carcinogenicity and mutagenicity were predicted. Trifluoromethyl indoles 10i and 10k showed extremely promising activities against WT HIV-1 with IC50 values at the low nanomolar level, similar to efavirenz, better than nevirapine, and also possessed higher potency towards the drug-resistant mutant strain Y181C than nevirapine. Preliminary SAR and docking studies of detailed binding mode provided some insights for discovery of more potent NNRTIs.
语种: 英语
相关网址: 查看原文
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/38981
Appears in Collections:中科院天然产物有机化学重点实验室_期刊论文

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作者单位: 1.中科院上海有机化学研究所
2.北京微生物流行病研究所
3.中科院上海高等研究院

Recommended Citation:
Jiang HX,Zhuang DM,Huang Y,et al. Design, synthesis, and biological evaluation of novel trifluoromethyl indoles as potent HIV-1 NNRTIs with an improved drug resistance profile[J]. Org. Biomol. Chem.,2014,12(21):3446-3458.
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