1194041-97-8Relevant articles and documents
ZnO-mediated regioselective C-arylsulfonylation of indoles: A facile solvent-free synthesis of 2- and 3-sulfonylindoles and preliminary evaluation of their activity against drug-resistant mutant HIV-1 reverse transcriptases (RTs)
Tocco, Graziella,Begala, Michela,Esposito, Francesca,Caboni, Pierluigi,Cannas, Valeria,Tramontano, Enzo
, p. 6237 - 6241 (2013/10/22)
A ZnO-mediated one-pot solvent-free protocol for the regioselective C-arylsulfonylation of indoles is described and some novel derivatives were tested on wild type and non-nucleoside inhibitor resistant K103N and Y181C HIV-1 reverse transcriptases (RTs).
Anti human immunodeficiency virus-1 (HIV-1) agents 3. Synthesis and in vitro anti-HIV-1 activity of some N-arylsulfonylindoles
Fan, Ling-Ling,Liu, Wu-Qing,Xu, Hui,Yang, Liu-Meng,Lv, Min,Zheng, Yong-Tang
experimental part, p. 797 - 800 (2010/02/27)
In order to find compounds with superior anti human immunodeficiency virus type 1 (HIV-1) activity, twelve simple N-arylsulfonylindoles (3a-l) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro for the first time. Several compounds demonstrated significant anti-HIV-1 activity, especially N-(3-nitrobenzene) sulfonyl-6-methylindole (3h) and N-(3-nitrobenzene)sulfonylindole (3i) showed the highest anti-HIV-1 activity with EC50 values of 0.26 and 0.74 μg/ml, and TI values of 543.78 and >270.27, respectively.