ArticleJournal of medicinal chemistry2020
Selectivity and Physicochemical Optimization of Repurposed Pyrazolo[1,5-
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Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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9citing papers in PubMed
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Who cites it
9 citing papers in PubMed.
- Integrated computational approaches for identification of potent pyrazole-based glycogen synthase kinase-3β (GSK-3β) inhibitors: 3D-QSAR, virtual screening, docking, MM/GBSA, EC, MD simulation studies.Molecular diversity · 2025Article
- A Data-Driven Perspective on Bioisostere Evaluation: Mapping the Benzene Bioisostere Landscape with BioSTAR.Journal of medicinal chemistry · 2025Review
- Pharmacophore Identification and Structure-Activity Relationship Analysis of a Series of Substituted Azaindoles as Inhibitors ofJournal of medicinal chemistry · 2024Article
- Aminopyridines in the development of drug candidates against protozoan neglected tropical diseases.Future medicinal chemistry · 2024Review
- Targeted protein degradation might present a novel therapeutic approach in the fight against African trypanosomiasis.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences · 2023Article
- Identification of novel anti-amoebic pharmacophores from kinase inhibitor chemotypes.Frontiers in microbiology · 2023Article
- Phenotypic drug discovery: recent successes, lessons learned and new directions.Nature reviews. Drug discovery · 2022Review
- Chemical Cartography Approaches to Study Trypanosomatid Infection.Journal of visualized experiments : JoVE · 2022Article
- Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors.Journal of medicinal chemistry · 2021Article
Corrections and comments
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Authors and funding
17 authors.
Westley F TearDepartment of Chemistry & Chemical Biology , Northeastern University , 360 Huntington Avenue , Boston , Massachusetts 02115 , United States.
Seema BagDepartment of Chemistry & Chemical Biology , Northeastern University , 360 Huntington Avenue , Boston , Massachusetts 02115 , United States.
Rosario Diaz-GonzalezInstituto de Parasitología y Biomedicina "López-Neyra", Consejo Superior de Investigaciones Cientificas (CSIC) , Granada 18016 , Spain.
Gloria Ceballos-PérezInstituto de Parasitología y Biomedicina "López-Neyra", Consejo Superior de Investigaciones Cientificas (CSIC) , Granada 18016 , Spain.
Domingo I Rojas-BarrosInstituto de Parasitología y Biomedicina "López-Neyra", Consejo Superior de Investigaciones Cientificas (CSIC) , Granada 18016 , Spain.
Carlos Cordon-ObrasInstituto de Parasitología y Biomedicina "López-Neyra", Consejo Superior de Investigaciones Cientificas (CSIC) , Granada 18016 , Spain.
Guiomar Pérez-MorenoInstituto de Parasitología y Biomedicina "López-Neyra", Consejo Superior de Investigaciones Cientificas (CSIC) , Granada 18016 , Spain.
Raquel García-HernándezInstituto de Parasitología y Biomedicina "López-Neyra", Consejo Superior de Investigaciones Cientificas (CSIC) , Granada 18016 , Spain.
Maria Santos Martinez-MartinezTres Cantos Medicines Development Campus, DDW and CIB , GlaxoSmithKline , Tres Cantos 28760 , Spain.
Luis Miguel Ruiz-PerezInstituto de Parasitología y Biomedicina "López-Neyra", Consejo Superior de Investigaciones Cientificas (CSIC) , Granada 18016 , Spain.
Francisco GamarroInstituto de Parasitología y Biomedicina "López-Neyra", Consejo Superior de Investigaciones Cientificas (CSIC) , Granada 18016 , Spain.
Dolores Gonzalez PacanowskaInstituto de Parasitología y Biomedicina "López-Neyra", Consejo Superior de Investigaciones Cientificas (CSIC) , Granada 18016 , Spain.
Conor R CaffreyCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences , University of California San Diego , 9500 Gilman Drive , La Jolla , California 92093 , United States.
Lori FerrinsDepartment of Chemistry & Chemical Biology , Northeastern University , 360 Huntington Avenue , Boston , Massachusetts 02115 , United States.ORCID 0000-0001-8992-0919
Pilar ManzanoTres Cantos Medicines Development Campus, DDW and CIB , GlaxoSmithKline , Tres Cantos 28760 , Spain.
Miguel NavarroInstituto de Parasitología y Biomedicina "López-Neyra", Consejo Superior de Investigaciones Cientificas (CSIC) , Granada 18016 , Spain.
Michael P PollastriDepartment of Chemistry & Chemical Biology , Northeastern University , 360 Huntington Avenue , Boston , Massachusetts 02115 , United States.ORCID 0000-0001-9943-7197
Funding
Optimization and Modes of Action of NEU-4438, a New Anti-trypanosome Lead DrugR01AI124046 · NIAID · NORTHEASTERN UNIVERSITY · PI FERRINS, LORI, MENSA-WILMOT, KOJO A. · 2016 to 2025
$6.0MRepurposing human kinase inhibitor chemotypes for Neglected Tropical DiseasesR01AI114685 · NIAID · NORTHEASTERN UNIVERSITY · PI FERRINS, LORI · 2015 to 2025
$4.6MValidation and development of trypanosomal phosphodiesterase inhibitors for treatR01AI082577 · NIAID · NORTHEASTERN UNIVERSITY · PI CAMPBELL, ROBERT KIRWAN, POLLASTRI, MICHAEL P · 2009 to 2013
$2.6MLead Optimization of Lapatinib Analogs for Human African TrypanosomiasisR56AI099476 · NIAID · UNIVERSITY OF GEORGIA · PI MENSA-WILMOT, KOJO A., POLLASTRI, MICHAEL P · 2014 to 2014
$672kLead optimization of agents targeting multiple kinetoplastid parasitesR21AI127594 · NIAID · NORTHEASTERN UNIVERSITY · PI POLLASTRI, MICHAEL P · 2017 to 2018
$427kDefining the death transcriptome of Schistosoma mansoni to construct a molecular drug screenR21AI126296 · NIAID · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI CAFFREY, CONOR · 2017 to 2018
$415kNIAID NIH HHS R01 AI082577NIAID NIH HHS R01 AI114685NIAID NIH HHS R01 AI124046NIAID NIH HHS R21 AI126296NIAID NIH HHS R21 AI127594NIAID NIH HHS R56 AI099476
Abstract
From a high-throughput screen of 42 444 known human kinases inhibitors, a pyrazolo[1,5-
Indexed as
AnimalsCell SurvivalCrystallography, X-RayCyclin-Dependent Kinase 2Cyclin-Dependent Kinase 4Drug RepositioningGlycogen Synthase Kinase 3 betaHepatocytesHigh-Throughput Screening AssaysHumansLeishmania donovaniMiceModels, MolecularPyridazinesRatsStructure-Activity RelationshipCDK2 protein, humanCDK4 protein, humanCyclin-Dependent Kinase 2Cyclin-Dependent Kinase 4Glycogen Synthase Kinase 3 betaPyridazinesTrypanocidal Agents
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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.