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

Jiang, Tao and Kuhen, Kelli and Wolff, Karen and Yin, Hong and Bieza, Kimberly and Caldwell, Jeremy and Bursulaya, Badry and Wu, Tom and He, Yun (2006) Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. Bioorganic & Medicinal Chemistry Letters, 16 (8). pp. 2105-2108. ISSN 0960-894X

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.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing)
Keywords: AIDS; HIV; Reverse transcriptase; Inhibitor; Oxindole; SAR
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Date Deposited: 14 Dec 2009 14:04
Last Modified: 31 Jan 2013 01:26
URI: https://oak.novartis.com/id/eprint/159

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