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

  • Bioorg Med Chem Lett. 2006 Apr 15;16(8):2105-8. doi: 10.1016/j.bmcl.2006.01.073.
Tao Jiang  1 ,  Kelli L Kuhen ,  Karen Wolff ,  Hong Yin ,  Kimberly Bieza ,  Jeremy Caldwell ,  Badry Bursulaya ,  Tom Yao-Hsing Wu ,  Yun He
Affiliations
  • 1. Genomics Institute of the Novartis Research Foundation (GNF), 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA.
PMID: 16480865 DOI: 10.1016/j.bmcl.2006.01.073
Abstract

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.