Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I

…, K Wolff, H Yin, K Bieza, J Caldwell, B Bursulaya…

文献索引：Jiang, Tao; Kuhen, Kelli L.; Wolff, Karen; Yin, Hong; Bieza, Kimberly; Caldwell, Jeremy; Bursulaya, Badry; Wu, Tom Yao-Hsing; He, Yun Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 8 p. 2105 - 2108

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被引用次数: 133

摘要

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.