Design, synthesis, and biological evaluation of novel trifluoromethyl indoles as potent HIV-1 NNRTIs with an improved drug resistance profile
文献类型：期刊论文
| 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 |
| 刊名 | Org. Biomol. Chem.
 |
| 出版日期 | 2014 |
| 卷号 | 12期号:21页码:3446-3458 |
| 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 |
| 通讯作者 | 张琛 ; 姜标 |
| 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. |
| 学科主题 | 天然产物有机化学 |
| 收录类别 | SCI |
| 原文出处 | http://dx.doi.org/10.1039/c3ob42186d |
| 语种 | 英语 |
| 源URL | [http://ir.sioc.ac.cn/handle/331003/38981]  |
| 专题 | 上海有机化学研究所_中科院天然产物有机化学重点实验室 |
| 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 |
| 推荐引用方式 GB/T 7714 | 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. |
| APA | 姜海霞.,庄道明.,黄迎.,曹欣欣.,姚建华.,...&姜标.(2014).Design, synthesis, and biological evaluation of novel trifluoromethyl indoles as potent HIV-1 NNRTIs with an improved drug resistance profile.Org. Biomol. Chem.,12(21),3446-3458. |
| MLA | 姜海霞,et al."Design, synthesis, and biological evaluation of novel trifluoromethyl indoles as potent HIV-1 NNRTIs with an improved drug resistance profile".Org. Biomol. Chem. 12.21(2014):3446-3458. |
入库方式： OAI收割
来源：上海有机化学研究所
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