ArticleJournal of medicinal chemistry2019
Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
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Article in Journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed.
- Antiviral drug discovery and development: challenges and future directions.Signal transduction and targeted therapy · 2026Review
- Development of enhanced HIV-1 non-nucleoside reverse transcriptase inhibitors with improved resistance and pharmacokinetic profiles.Science advances · 2025Article
- Sulfoxidation of pyrimidine thioate derivatives and study their biological activities.Scientific reports · 2025Article
- Transition-Metal Catalyzed Synthesis of Pyrimidines: Recent Advances, Mechanism, Scope and Future Perspectives.Topics in current chemistry (Cham) · 2024Review
- Strategies in the Design and Development of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs).Viruses · 2023Review
- Review
- Article
- Article
- Development of fluorine-substituted NHActa pharmaceutica Sinica. B · 2023Article
- Design and Synthesis of Novel HIV-1 NNRTIs with Bicyclic Cores and with Improved Physicochemical Properties.Journal of medicinal chemistry · 2023Article
- Covalently Targeted Highly Conserved Tyr318 to Improve the Drug Resistance Profiles of HIV-1 NNRTIs: A Proof-of-Concept Study.International journal of molecular sciences · 2023Article
- DEEPCYPs: A deep learning platform for enhanced cytochrome P450 activity prediction.Frontiers in pharmacology · 2023Article
- Identification of Boronate-Containing Diarylpyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors.Molecules (Basel, Switzerland) · 2022Article
- Newly Emerging Strategies in Antiviral Drug Discovery: Dedicated to Prof. Dr. Erik De Clercq on Occasion of His 80th Anniversary.Molecules (Basel, Switzerland) · 2022Review
- Thienopyrimidine: A Promising Scaffold to Access Anti-Infective Agents.Pharmaceuticals (Basel, Switzerland) · 2021Review
- 2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.Journal of medicinal chemistry · 2021Article
- Structure-based non-nucleoside inhibitor design: Developing inhibitors that are effective against resistant mutants.Chemical biology & drug design · 2021Article
- Development of non-nucleoside reverse transcriptase inhibitors (NNRTIs): our past twenty years.Acta pharmaceutica Sinica. B · 2020Review
- Exploring the hydrophobic channel of NNIBP leads to the discovery of novel piperidine-substituted thiophene[3,2-Acta pharmaceutica Sinica. B · 2020Article
- Evolving understanding of HIV-1 reverse transcriptase structure, function, inhibition, and resistance.Current opinion in structural biology · 2020Review
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Authors and funding
19 authors.
Dongwei KangDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , 44 West Culture Road , 250012 Jinan , Shandong , P. R. China.ORCID 0000-0001-9232-953X
Heng ZhangDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , 44 West Culture Road , 250012 Jinan , Shandong , P. R. China.
Zhao WangDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , 44 West Culture Road , 250012 Jinan , Shandong , P. R. China.
Tong ZhaoDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , 44 West Culture Road , 250012 Jinan , Shandong , P. R. China.
Tiziana GinexDepartment of Nutrition, Food Science and Gastronomy, Faculty of Pharmacy, Campus Torribera, Institute of Biomedicine (IBUB) and Institute of Theoretical and Computational Chemistry (IQTCUB) , University of Barcelona , 08921 Santa Coloma de Gramenet , Spain.
Francisco Javier LuqueDepartment of Nutrition, Food Science and Gastronomy, Faculty of Pharmacy, Campus Torribera, Institute of Biomedicine (IBUB) and Institute of Theoretical and Computational Chemistry (IQTCUB) , University of Barcelona , 08921 Santa Coloma de Gramenet , Spain.ORCID 0000-0002-8049-3567
Yang YangDepartment of Molecular Biophysics and Biochemistry , Yale University , New Haven , Connecticut 06520-8114 , United States.
Gaochan WuDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , 44 West Culture Road , 250012 Jinan , Shandong , P. R. China.
Da FengDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , 44 West Culture Road , 250012 Jinan , Shandong , P. R. China.
Fenju WeiDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , 44 West Culture Road , 250012 Jinan , Shandong , P. R. China.
Jian ZhangDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , 44 West Culture Road , 250012 Jinan , Shandong , P. R. China.ORCID 0000-0002-5668-2974
Erik De ClercqLaboratory of Virology and Chemotherapy, Rega Institute for Medical Research , KU Leuven , Herestraat 49 Postbus 1043 (09.A097) , B-3000 Leuven , Belgium.
Christophe PannecouqueLaboratory of Virology and Chemotherapy, Rega Institute for Medical Research , KU Leuven , Herestraat 49 Postbus 1043 (09.A097) , B-3000 Leuven , Belgium.
Chin Ho ChenSurgical Oncology Research Facility , Duke University Medical Center , Box 2926, Durham , North Carolina 27710 , United States.
Kuo-Hsiung LeeNatural Products Research Laboratories, Eshelman School of Pharmacy , University of North Carolina , Chapel Hill , North Carolina 27599 , United States.ORCID 0000-0002-6562-0070
N Arul MuruganDepartment of Theoretical Chemistry and Biology, Royal Institute of Technology (KTH) , AlbaNova University Center , S-106 91 Stockholm , Sweden.
Thomas A SteitzDepartment of Molecular Biophysics and Biochemistry , Yale University , New Haven , Connecticut 06520-8114 , United States.
Peng ZhanDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , 44 West Culture Road , 250012 Jinan , Shandong , P. R. China.ORCID 0000-0002-9675-6026
Xinyong LiuDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , 44 West Culture Road , 250012 Jinan , Shandong , P. R. China.
Funding
PLANT ANTIHIV AGENTSR01AI033066 · NIAID · UNIV OF NORTH CAROLINA CHAPEL HILL · PI LEE, KUO-HSIUNG · 1992 to 2018
$8.4MNIAID NIH HHS R01 AI033066
Abstract
To address drug resistance to HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs), a series of novel diarylpyrimidine (DAPY) derivatives targeting "tolerant region I" and "tolerant region II" of the NNRTIs binding pocket (NNIBP) were designed utilizing a structure-guided scaffold-hopping strategy. The dihydrofuro[3,4- d]pyrimidine derivatives 13c2 and 13c4 proved to be exceptionally potent against a wide range of HIV-1 strains carrying single NNRTI-resistant mutations (EC
Indexed as
AnimalsAnti-HIV AgentsBinding SitesCell Line, TumorFuransHIV-1HIV Reverse TranscriptaseHumansMaleMicrobial Sensitivity TestsMolecular Dynamics SimulationMolecular StructurePyrimidinesRats, WistarReverse Transcriptase InhibitorsStructure-Activity RelationshipAnti-HIV AgentsFuransHIV Reverse TranscriptasePyrimidinesreverse transcriptase, Human immunodeficiency virus 1Reverse Transcriptase Inhibitors
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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.