943411-99-2Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of novel trifluoromethyl indoles as potent HIV-1 NNRTIs with an improved drug resistance profile
Jiang, Hai-Xia,Zhuang, Dao-Min,Huang, Ying,Cao, Xing-Xin,Yao, Jian-Hua,Li, Jing-Yun,Wang, Jian-Yong,Zhang, Chen,Jiang, Biao
, p. 3446 - 3458 (2014/05/20)
A 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. the Partner Organisations 2014.
