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Recently, we reported the racemic synthesis of 3'-fluoro-5'-norcarbocyclic nucleoside phosphonates bearing adenine as the heterocyclic base. For this study, to evaluate the antiviral activity of each enantiomer, we synthesized both enantiomers, as well as their corresponding bis(POM) prodrugs. Anti-HIV-1 evaluation against the LAI strain and clinically NRTI-resistant HIV-1 strains are presented. The activities against these different strains show that the activities of bis(POM) prodrug (-)-9 are equivalent or even superior to those of (R)-PMPA.
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http://dx.doi.org/10.1002/cmdc.202200377 | DOI Listing |
ACS Omega
June 2025
Department of Pharmaceutical Sciences, Universidad de Navarra, Pamplona 31008, Spain.
Human African trypanosomiasis (HAT) is caused by Trypanosoma brucei. Drug therapy remains challenging due to drug resistance and/or toxicity. New drugs are needed.
View Article and Find Full Text PDFCancer Lett
December 2024
Shandong Provincial Key Laboratory of Clinical Research for Pancreatic Diseases, Tumor Immunology and Cytotherapy, Medical Research Center, The Affiliated Hospital of Qingdao University, Qingdao, 266000, China; Gastrointestinal Cancer Institute/Pancreatic Disease Institute, The Affiliated Hospital o
Pancreatic ductal adenocarcinoma (PDAC) is a deadly cancer known for its high rate of early metastasis, necessitating the discovery of the underlying mechanisms. Herein, we report that heterogeneous nuclear ribonucleoprotein L-like (hnRNPLL) expression significantly increases at the invasion forefront in PDAC and is associated with early metastasis and poor prognosis. Our findings revealed that hnRNPLL knockdown resulted in extensive exon skipping (ES) events.
View Article and Find Full Text PDFEur J Med Chem
February 2025
Biological and Molecular Chemistry Research Group, Institute of Chemistry and Biotechnology, Federal University of Alagoas, Lourival Melo Mota Avenue, AC. Simões Campus, Alagoas, Maceió, 57072-970, Brazil. Electronic address:
Trypanosoma cruzi (T. cruzi) and Trypanosoma brucei (T. brucei) urgently demand innovative drug development due to their impact on public health worldwide.
View Article and Find Full Text PDFChemMedChem
October 2022
Institut des Biomolécules Max Mousseron (IBMM), UMR 5247, Université de Montpellier, CNRS, ENSCM, 1019, route de Mende, 34293, Montpellier, France.
Recently, we reported the racemic synthesis of 3'-fluoro-5'-norcarbocyclic nucleoside phosphonates bearing adenine as the heterocyclic base. For this study, to evaluate the antiviral activity of each enantiomer, we synthesized both enantiomers, as well as their corresponding bis(POM) prodrugs. Anti-HIV-1 evaluation against the LAI strain and clinically NRTI-resistant HIV-1 strains are presented.
View Article and Find Full Text PDFFront Microbiol
April 2022
Department of Biological Sciences, Texas Tech University, Lubbock, TX, United States.
is a widespread endosymbiont of insects and filarial nematodes that profoundly influences host biology. has also been reported in rhizosphere hosts, where its diversity and function remain poorly characterized. The discovery that plant-parasitic nematodes (PPNs) host strains with unknown roles is of interest evolutionarily, ecologically, and for agriculture as a potential target for developing new biological controls.
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