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Design, synthesis, and biological evaluation of novel trifluoromethyl indoles as potent HIV-1 NNRTIs with an improved drug resistance profile
Alternative Title新型三氟甲基吲哚类HIV-1 NNRTIs的设计、合成及活性研究
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
2014
Source PublicationOrg. Biomol. Chem.
Volume12Issue:21Pages:3446-3458
Abstractnovel 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.
Subject Area天然产物有机化学
DOI10.1039/c3ob42186d
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Indexed BySCI
Language英语
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Document Type期刊论文
Identifierhttp://ir.sioc.ac.cn/handle/331003/38981
Collection中科院天然产物有机化学重点实验室
Corresponding AuthorZhang C(张琛); Jiang B(姜标)
Affiliation1.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
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.
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