Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I
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- 作者：Tao Jiang ; Kelli L. Kuhen ; Karen Wolff ; Hong Yin ; Kimberly Bieza ; Jeremy Caldwell ; Badry Bursulaya ; Tom Yao-Hsing Wu and Yun He
- 关键词：AIDS ; HIV ; Reverse transcriptase ; Inhibitor ; Oxindole ; SAR
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2006
- 出版时间：15 April 2006
- 年：2006
- 卷：16
- 期：8
- 页码：2105-2108
- 全文大小：149 K
文摘
A novel oxindole was discovered as an HIV non-nucleoside reverse transcriptase inhibitor via HTS using a cell-based assay. Systematic structural modifications were carried out to establish its SAR. These modifications led to the identification of oxindoles with low nanomolar potency for inhibiting HIV replication. These novel and potent oxindoles could serve as advanced leads for further optimizations.