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2009:
Fan Ling-Ling; Liu Wu-Qing; Xu Hui; Yang Liu-Meng; Lv Min; Zheng Yong-Tang
Anti human immunodeficiency virus-1 (HIV-1) agents 3. synthesis and in vitro anti-HIV-1 activity of some N-arylsulfonylindoles.
Chemical & pharmaceutical bulletin 2009;
57(
8):.
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 EC(50) values of 0.26 and 0.74 microg/ml, and TI values of 543.78 and >270.27, respectively.
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