Small molecule inhibitors of HIV RT Ribonuclease H

Small molecule inhibitors of HIV RT Ribonuclease H
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DOI:
10.1016/j.bmcl.2009.10.043
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发表时间:
2010-01-01
影响因子:
2.7
通讯作者:
O'Connell, John
O'Connell, John
中科院分区:
医学4区
文献类型:
--
作者:
Di Grandi, Martin;Olson, Matthew;O'Connell, John

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Two classes of compounds, thiocarbamates 1 and triazoles 2, have been identified as HIV RT RNase H inhibitors using a novel FRET-based HTS assay. The potent analogs in each series exhibited selectivity and were active in cell-based assays. In addition, saturable, 1: 1 stoichiometric binding to target was established and time of addition studies were consistent with inhibition of RT-mediated HIV replication. (C) 2009 Elsevier Ltd. All rights reserved.