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Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors.
Singh, Baljinder; Bernatchez, Jean A; McCall, Laura-Isobel; Calvet, Claudia M; Ackermann, Jasmin; Souza, Julia M; Thomas, Diane; Silva, Everton M; Bachovchin, Kelly A; Klug, Dana M; Jalani, Hitesh B; Bag, Seema; Buskes, Melissa J; Leed, Susan E; Roncal, Norma E; Penn, Erica C; Erath, Jessey; Rodriguez, Ana; Sciotti, Richard J; Campbell, Robert F; McKerrow, James; Siqueira-Neto, Jair L; Ferrins, Lori; Pollastri, Michael P.
  • Singh B; Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
  • Bernatchez JA; Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
  • McCall LI; Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
  • Calvet CM; Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
  • Ackermann J; Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
  • Souza JM; Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
  • Thomas D; Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
  • Silva EM; Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
  • Bachovchin KA; Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
  • Klug DM; Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
  • Jalani HB; Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
  • Bag S; Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
  • Buskes MJ; Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
  • Leed SE; Experimental Therapeutics, Walter Reed Army Institute of Research, 2460 Linden Lane, Silver Spring, Maryland 20910, United States.
  • Roncal NE; Experimental Therapeutics, Walter Reed Army Institute of Research, 2460 Linden Lane, Silver Spring, Maryland 20910, United States.
  • Penn EC; Experimental Therapeutics, Walter Reed Army Institute of Research, 2460 Linden Lane, Silver Spring, Maryland 20910, United States.
  • Erath J; Department of Microbiology, New York University School of Medicine, 430 East 29th Street, New York, New York 10010, United States.
  • Rodriguez A; Department of Microbiology, New York University School of Medicine, 430 East 29th Street, New York, New York 10010, United States.
  • Sciotti RJ; Experimental Therapeutics, Walter Reed Army Institute of Research, 2460 Linden Lane, Silver Spring, Maryland 20910, United States.
  • Campbell RF; Experimental Therapeutics, Walter Reed Army Institute of Research, 2460 Linden Lane, Silver Spring, Maryland 20910, United States.
  • McKerrow J; Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
  • Siqueira-Neto JL; Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
  • Ferrins L; Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
  • Pollastri MP; Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
ACS Med Chem Lett ; 11(3): 249-257, 2020 Mar 12.
Article en En | MEDLINE | ID: mdl-32184953
ABSTRACT
Utilizing a target repurposing and parasite-hopping approach, we tested a previously reported library of compounds that were active against Trypanosoma brucei, plus 31 new compounds, against a variety of protozoan parasites including Trypanosoma cruzi, Leishmania major, Leishmania donovani, and Plasmodium falciparum. This led to the discovery of several compounds with submicromolar activities and improved physicochemical properties that are early leads toward the development of chemotherapeutic agents against kinetoplastid diseases and malaria.
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Texto completo: 1 Banco de datos: MEDLINE Idioma: En Año: 2020 Tipo del documento: Article
Texto completo
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XML
PubMed Links
Search on Google

Texto completo: 1 Banco de datos: MEDLINE Idioma: En Año: 2020 Tipo del documento: Article