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

Tao Jiang; Kelli L Kuhen; Karen Wolff; Hong Yin; Kimberly Bieza; Jeremy Caldwell; Badry Bursulaya; Tom Yao-Hsing Wu; Yun He

doi:10.1016/j.bmcl.2006.01.073

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. Epub 2006 Feb 9.

Authors

Tao Jiang¹, Kelli L Kuhen, Karen Wolff, Hong Yin, Kimberly Bieza, Jeremy Caldwell, Badry Bursulaya, Tom Yao-Hsing Wu, Yun He

Affiliation

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.

Publication types

Evaluation Study

MeSH terms

Anti-HIV Agents / chemical synthesis
Anti-HIV Agents / pharmacology
Drug Resistance, Viral
HIV-1 / drug effects*
Indoles / chemical synthesis
Indoles / pharmacology
Reverse Transcriptase Inhibitors / chemical synthesis*
Reverse Transcriptase Inhibitors / pharmacology*
Stereoisomerism
Structure-Activity Relationship
Virus Replication

Substances

Anti-HIV Agents
Indoles
Reverse Transcriptase Inhibitors