ArticleJournal of medicinal chemistry2008
A copper(I)-catalyzed 1,2,3-triazole azide-alkyne click compound is a potent inhibitor of a multidrug-resistant HIV-1 protease variant.
Article in Journal of medicinal chemistry, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers.
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Who cites it
36 citing papers in PubMed, 242 citations in OpenAlex.
- Exploring the versatility of heterocyclic compounds containing nitrogen atoms (triazoles): a comprehensive review.RSC advances · 2025Review
- Evaluation of novel nitrophenol-triazole hybrid molecules: biological screening and computational profiling.Future medicinal chemistry · 2025Article
- Synthesis, antidiabetic activity and molecular docking studies of novel aryl benzylidenethiazolidine-2,4-dione based 1,2,3-triazoles.Molecular diversity · 2024Article
- A Literature Review Focusing on the Antiviral Activity of [1,2,4] and [1,2,3]-triazoles.Mini reviews in medicinal chemistry · 2024Review
- Click Triazole as a Linker for Pretargeting Strategies: Synthesis, Docking Investigations, Fluorescence Diagnosis, and Antibacterial Action Studies.Molecules (Basel, Switzerland) · 2023Article
- Mechanochemical Approach towards Multi-Functionalized 1,2,3-Triazoles and Anti-Seizure Drug Rufinamide Analogs Using Copper Beads.Molecules (Basel, Switzerland) · 2022Article
- Silver-Catalyzed Cascade Cyclization of Amino-Molecules (Basel, Switzerland) · 2022Article
- Design of new bis-triazolyl structure for identification of inhibitory activity on COVID-19 main protease by molecular docking approach.Journal of molecular structure · 2022Article
- Synthesis and Evaluation of Biphenyl-1,2,3-Triazol-Benzonitrile Derivatives as PD-1/PD-L1 Inhibitors.ACS omega · 2020Article
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- Synthesis and cytotoxic effect of a fewResearch in pharmaceutical sciences · 2020Article
- CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review.RSC advances · 2020Review
- Crystal structure, computational study and Hirshfeld surface analysis of ethyl (2Acta crystallographica. Section E, Crystallographic communications · 2019Article
- NewRSC advances · 2019Article
- Synthesis of Triazole-Substituted Quinazoline Hybrids for Anticancer Activity and a Lead Compound as the EGFR Blocker and ROS Inducer Agent.ACS omega · 2018Article
- Synthesis and antibacterial activity of new 1,2,3-triazolylmethyl-2H-1,4-benzothiazin-3(4H)-one derivatives.Chemistry Central journal · 2018Article
- Conventional and microwave-assisted synthesis of new indole-tethered benzimidazole-based 1,2,3-triazoles and evaluation of their antimycobacterial, antioxidant and antimicrobial activities.Molecular diversity · 2018Article
- Recent trends in click chemistry as a promising technology for virus-related research.Virus research · 2018Review
- Crystal structure analysis of [5-(4-meth-oxy-phen-yl)-2-methyl-2Acta crystallographica. Section E, Crystallographic communications · 2018Article
Corrections and comments
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Authors and funding
10 authors at 1 institution in 1 country.
Funding
Abstract
Treatment with HIV-1 protease inhibitors, a component of highly active antiretroviral therapy (HAART), often results in viral resistance. Structural and biochemical characterization of a 6X protease mutant arising from in vitro selection with compound 1, a C 2-symmetric diol protease inhibitor, has been previously described. We now show that compound 2, a copper(I)-catalyzed 1,2,3-triazole derived compound previously shown to be potently effective against wild-type protease (IC 50 = 6.0 nM), has low nM activity (IC 50 = 15.7 nM) against the multidrug-resistant 6X protease mutant. Compound 2 displays similar efficacy against wild-type and 6X HIV-1 in viral replication assays. While structural studies of compound 1 bound to wild type and mutant proteases revealed a progressive change in binding mode in the mutants, the 1.3 A resolution 6X protease-compound 2 crystal structure reveals nearly identical interactions for 2 as in the wild-type protease complex with very little change in compound 2 or protease conformation.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.