BIOMAT Database Logo BIOMAT Database Logo

Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I. 2006

Tao Jiang, and Kelli L Kuhen, and Karen Wolff, and Hong Yin, and Kimberly Bieza, and Jeremy Caldwell, and Badry Bursulaya, and Tom Yao-Hsing Wu, and Yun He
Genomics Institute of the Novartis Research Foundation (GNF), 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA.

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.

UI MeSH Term Description Entries
D007211 Indoles Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
D013237 Stereoisomerism The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed) Molecular Stereochemistry,Stereoisomers,Stereochemistry, Molecular,Stereoisomer
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D014779 Virus Replication The process of intracellular viral multiplication, consisting of the synthesis of PROTEINS; NUCLEIC ACIDS; and sometimes LIPIDS, and their assembly into a new infectious particle. Viral Replication,Replication, Viral,Replication, Virus,Replications, Viral,Replications, Virus,Viral Replications,Virus Replications
D015497 HIV-1 The type species of LENTIVIRUS and the etiologic agent of AIDS. It is characterized by its cytopathic effect and affinity for the T4-lymphocyte. Human immunodeficiency virus 1,HIV-I,Human Immunodeficiency Virus Type 1,Immunodeficiency Virus Type 1, Human
D018894 Reverse Transcriptase Inhibitors Inhibitors of reverse transcriptase (RNA-DIRECTED DNA POLYMERASE), an enzyme that synthesizes DNA on an RNA template. Reverse Transcriptase Inhibitor,Inhibitors, Reverse Transcriptase,Inhibitor, Reverse Transcriptase,Transcriptase Inhibitor, Reverse
D019380 Anti-HIV Agents Agents used to treat AIDS and/or stop the spread of the HIV infection. These do not include drugs used to treat symptoms or opportunistic infections associated with AIDS. AIDS Drug,AIDS Drugs,Anti-AIDS Agents,Anti-AIDS Drug,Anti-HIV Agent,Anti-HIV Drug,Anti-AIDS Drugs,Anti-HIV Drugs,Agent, Anti-HIV,Agents, Anti-AIDS,Agents, Anti-HIV,Anti AIDS Agents,Anti AIDS Drug,Anti AIDS Drugs,Anti HIV Agent,Anti HIV Agents,Anti HIV Drug,Anti HIV Drugs,Drug, AIDS,Drug, Anti-AIDS,Drug, Anti-HIV,Drugs, AIDS,Drugs, Anti-AIDS,Drugs, Anti-HIV
D024882 Drug Resistance, Viral The ability of viruses to resist or to become tolerant to chemotherapeutic agents or antiviral agents. This resistance is acquired through gene mutation. Antiviral Drug Resistance,Antiviral Drug Resistances,Drug Resistances, Viral

Related Publications

Tao Jiang, and Kelli L Kuhen, and Karen Wolff, and Hong Yin, and Kimberly Bieza, and Jeremy Caldwell, and Badry Bursulaya, and Tom Yao-Hsing Wu, and Yun He
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
August 2006, Bioorganic & medicinal chemistry letters,
Tao Jiang, and Kelli L Kuhen, and Karen Wolff, and Hong Yin, and Kimberly Bieza, and Jeremy Caldwell, and Badry Bursulaya, and Tom Yao-Hsing Wu, and Yun He
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
August 2006, Bioorganic & medicinal chemistry letters,
Tao Jiang, and Kelli L Kuhen, and Karen Wolff, and Hong Yin, and Kimberly Bieza, and Jeremy Caldwell, and Badry Bursulaya, and Tom Yao-Hsing Wu, and Yun He
Arylazolylthioacetanilide. Part 11: design, synthesis and biological evaluation of 1,2,4-triazole thioacetanilide derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
November 2013, Medicinal chemistry (Shariqah (United Arab Emirates)),
Tao Jiang, and Kelli L Kuhen, and Karen Wolff, and Hong Yin, and Kimberly Bieza, and Jeremy Caldwell, and Badry Bursulaya, and Tom Yao-Hsing Wu, and Yun He
Design and synthesis of novel oxindoles as potential non-nucleosidic reverse transcriptase inhibitors against HIV.
January 2008, Nucleic acids symposium series (2004),
Tao Jiang, and Kelli L Kuhen, and Karen Wolff, and Hong Yin, and Kimberly Bieza, and Jeremy Caldwell, and Badry Bursulaya, and Tom Yao-Hsing Wu, and Yun He
Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
August 2009, Bioorganic & medicinal chemistry,
Tao Jiang, and Kelli L Kuhen, and Karen Wolff, and Hong Yin, and Kimberly Bieza, and Jeremy Caldwell, and Badry Bursulaya, and Tom Yao-Hsing Wu, and Yun He
Rational design and synthesis of novel thiazolidin-4-ones as non-nucleoside HIV-1 reverse transcriptase inhibitors.
June 2014, Bioorganic & medicinal chemistry,
Tao Jiang, and Kelli L Kuhen, and Karen Wolff, and Hong Yin, and Kimberly Bieza, and Jeremy Caldwell, and Badry Bursulaya, and Tom Yao-Hsing Wu, and Yun He
[Design, synthesis and biologic evaluation of diarylbenzimidazole derivatives as novel HIV-1 non-nucleoside reverse transcriptase inhibitors].
November 2009, Yao xue xue bao = Acta pharmaceutica Sinica,
Tao Jiang, and Kelli L Kuhen, and Karen Wolff, and Hong Yin, and Kimberly Bieza, and Jeremy Caldwell, and Badry Bursulaya, and Tom Yao-Hsing Wu, and Yun He
Synthesis and biological evaluation of aryl-phospho-indole as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
January 2011, Journal of medicinal chemistry,
Tao Jiang, and Kelli L Kuhen, and Karen Wolff, and Hong Yin, and Kimberly Bieza, and Jeremy Caldwell, and Badry Bursulaya, and Tom Yao-Hsing Wu, and Yun He
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
February 2004, Journal of medicinal chemistry,
Tao Jiang, and Kelli L Kuhen, and Karen Wolff, and Hong Yin, and Kimberly Bieza, and Jeremy Caldwell, and Badry Bursulaya, and Tom Yao-Hsing Wu, and Yun He
Design and synthesis of novel distamycin-modified nucleoside analogues as HIV-1 reverse transcriptase inhibitors.
February 2014, Antiviral research,
Copied contents to your clipboard!