新型氧化吲哚作为HIV-1非核苷类逆转录酶抑制剂的设计、合成及生物学评价。第一部分。
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
作者信息
Jiang Tao, Kuhen Kelli L, Wolff Karen, Yin Hong, Bieza Kimberly, Caldwell Jeremy, Bursulaya Badry, Wu Tom Yao-Hsing, He Yun
机构信息
Genomics Institute of the Novartis Research Foundation (GNF), 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2006 Apr 15;16(8):2105-8. doi: 10.1016/j.bmcl.2006.01.073. Epub 2006 Feb 9.
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.
通过基于细胞的检测的高通量筛选，发现了一种新型氧化吲哚作为HIV非核苷逆转录酶抑制剂。进行了系统的结构修饰以确定其构效关系。这些修饰导致鉴定出对HIV复制具有低纳摩尔效力的氧化吲哚。这些新型强效氧化吲哚可作为进一步优化的高级先导化合物。
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