Results 121 to 130 of about 1,267 (159)

Discovery of arylsulfonamides as a novel class of allosteric integrase inhibitors with antiviral activity

Bioorganic & Medicinal Chemistry Letters, 2023
Lens epithelial-derived growth factor (LEDGF) increases the efficiency of proviral DNA integration into the host genome by interacting with HIV integrase (IN) and directing it to a chromatin environment that favors viral transcription. Allosteric integrase inhibitors (ALLINIs), such as known 2-(tert-butoxy)acetic acid (1), bind to the LEDGF pocket on ...
Cheng Wang, Gregory C. Adam, Christine Burlein, Steven Carroll, William Dankulich, Tracy Diamond, Jay Grobler, Jeffrey Heath, Adam Johnson, Daniel Klein, Daniel Krosky, Kartik Narayan, Yangsi Ou, John Sanders, Sujata Sharma, Min Xu, Antonella Converso   +16 more
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ChemInform Abstract: Allosteric Inhibitor Development Targeting HIV‐1 Integrase

ChemInform, 2011
AbstractReview: 95 refs.
Laith Q. Al‐Mawsawi, Nouri Neamati
openaire   +1 more source

Discovery of novel integrase-LEDGF/p75 allosteric inhibitors based on a benzene scaffold

Bioorganic & Medicinal Chemistry, 2020
We report herein the discovery of novel integrase-LEDGF/p75 allosteric inhibitors (INLAIs) based on a benzene scaffold 3. This scaffold can extend substituents from the C1 position unlike the common pyridine scaffolds 2. Structure-activity relationship studies showed that the sulfonamide linker at the C1 position was important for the antiviral ...
Shuichi, Sugiyama, Tsutomu, Iwaki, Yoshinori, Tamura, Kenji, Tomita, Eriko, Matsuoka, Shuhei, Arita, Takahiro, Seki, Tomokazu, Yoshinaga, Takashi, Kawasuji   +8 more
openaire   +2 more sources

Discovery of tricyclic HIV-1 integrase-LEDGF/p75 allosteric inhibitors by intramolecular direct arylation reaction

Bioorganic & Medicinal Chemistry Letters, 2022
We have been conducting exploratory research to develop human immunodeficiency virus type-1 (HIV-1) integrase-LEDGF/p75 allosteric inhibitors (INLAIs). Here, we report on a newly designed compound with a tricyclic scaffold that shows promise as an inhibitor.
Yoshiyuki, Taoda, Toshiyuki, Akiyama, Kenji, Tomita, Misato, Fujiwara-Kitamura, Yoshinori, Tamura, Takashi, Kawasuji, Eriko, Matsuoka, Erika, Akihisa, Takahiro, Seki, Tomokazu, Yoshinaga   +9 more
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Scaffold modifications to the 4-(4,4-dimethylpiperidinyl) 2,6-dimethylpyridinyl class of HIV-1 allosteric integrase inhibitors

Bioorganic & Medicinal Chemistry, 2022
Allosteric integrase inhibitors (ALLINIs) of HIV-1 may hold promise as a novel mechanism for HIV therapeutics and cure. Scaffold modifications to the 4-(4,4-dimethylpiperidinyl) 2,6-dimethylpyridinyl class of ALLINIs provided a series of potent compounds with differentiated 5/6 fused ring systems.
Kyle, Parcella, Manoj, Patel, Yong, Tu, Kyle, Eastman, Kevin, Peese, Eric, Gillis, Makonen, Belema, Ira B, Dicker, Brian, McAuliffe, Bo, Ding, Paul, Falk, Jean, Simmermacher, Dawn D, Parker, Prasanna, Sivaprakasam, Javed A, Khan, Kevin, Kish, Hal, Lewis, Umesh, Hanumegowda, Susan, Jenkins, John F, Kadow, Mark, Krystal, Nicholas A, Meanwell, B Narasimhulu, Naidu   +22 more
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Kuwanon‐L as a New Allosteric HIV‐1 Integrase Inhibitor: Molecular Modeling and Biological Evaluation

ChemBioChem, 2015
AbstractHIV‐1 integrase (IN) active site inhibitors are the latest class of drugs approved for HIV treatment. The selection of IN strand‐transfer drug‐resistant HIV strains in patients supports the development of new agents that are active as allosteric IN inhibitors.
Esposito, Francesca, Tintori, Cristina, Martini, Riccardo, Christ, Frauke, Debyser, Zeger, Ferrarese, Roberto, Cabiddu, Gianluigi, Corona, Angela, Ceresola, Elisa Rita, CALCATERRA, ANDREA, IOVINE, VALENTINA, BOTTA, Bruno, Clementi, Massimo, Canducci, Filippo, Botta, Maurizio, Tramontano, Enzo   +15 more
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5,6,7,8-Tetrahydro-1,6-naphthyridine Derivatives as Potent HIV-1-Integrase-Allosteric-Site Inhibitors

Journal of Medicinal Chemistry, 2019
A series of 5,6,7,8-tetrahydro-1,6-naphthyridine derivatives targeting the allosteric lens-epithelium-derived-growth-factor-p75 (LEDGF/p75)-binding site on HIV-1 integrase, an attractive target for antiviral chemotherapy, was prepared and screened for activity against HIV-1 infection in cell culture.
Kevin M. Peese, Christopher W. Allard, Timothy Connolly, Barry L. Johnson, Chen Li, Manoj Patel, Margaret E. Sorensen, Michael A. Walker, Nicholas A. Meanwell, Brian McAuliffe, Beatrice Minassian, Mark Krystal, Dawn D. Parker, Hal A. Lewis, Kevin Kish, Ping Zhang, Robert T. Nolte, Jean Simmermacher, Susan Jenkins, Christopher Cianci, B. Narasimhulu Naidu   +20 more
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Rational design of LEDGINs as first allosteric integrase inhibitors for the treatment of HIV infection

Drug Discovery Today: Technologies, 2013
The interaction between lens epithelium-derived growth factor (LEDGF/p75) and HIV-1 integrase (IN) is an attractive target for antiviral development because its inhibition blocks HIV replication. Developing novel small molecules that disrupt the LEDGF/p75-IN interaction constitutes a promising new therapeutic strategy for the treatment of HIV.
Belete A, Desimmie, Jonas, Demeulemeester, Frauke, Christ, Zeger, Debyser   +3 more
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