• myGriffith
    • Staff portal
    • Contact Us⌄
      • Future student enquiries 1800 677 728
      • Current student enquiries 1800 154 055
      • International enquiries +61 7 3735 6425
      • General enquiries 07 3735 7111
      • Online enquiries
      • Staff phonebook
    View Item 
    •   Home
    • Griffith Research Online
    • Journal articles
    • View Item
    • Home
    • Griffith Research Online
    • Journal articles
    • View Item
    JavaScript is disabled for your browser. Some features of this site may not work without it.

    Browse

  • All of Griffith Research Online
    • Communities & Collections
    • Authors
    • By Issue Date
    • Titles
  • This Collection
    • Authors
    • By Issue Date
    • Titles
  • Statistics

  • Most Popular Items
  • Statistics by Country
  • Most Popular Authors
  • Support

  • Contact us
  • FAQs
  • Admin login

  • Login
  • Open Source Drug Discovery: Highly Potent Antimalarial Compounds Derived from the Tres Cantos Arylpyrroles

    Thumbnail
    View/Open
    AveryPUB1680.pdf (715.5Kb)
    File version
    Version of Record (VoR)
    Author(s)
    Williamson, Alice E
    Ylioja, Paul M
    Robertson, Murray N
    Antonova-Koch, Yevgeniya
    Avery, Vicky
    Baell, Jonathan B
    Batchu, Harikrishna
    Batra, Sanjay
    Burrows, Jeremy N
    Bhattacharyya, Soumya
    Calderon, Felix
    Charman, Susan A
    Clark, Julie
    Crespo, Benigno
    Dean, Matin
    Debbert, Stefan L
    Delves, Michael
    Dennis, Adelaide SM
    Deroose, Frederik
    Duffy, Sandra
    Fletcher, Sabine
    Giaever, Guri
    Hallyburton, Irene
    Gamo, Francisco-Javier
    Gebbia, Marinella
    Guy, R Kiplin
    Hungerford, Zoe
    Kirk, Kiaran
    Lafuente-Monasterio, Maria J
    Lee, Anna
    Meister, Stephan
    Nislow, Corey
    Overington, John P
    Papadatos, George
    Patiny, Luc
    Pham, James
    Ralph, Stuart A
    Ruecker, Andrea
    Ryan, Eileen
    Southan, Christopher
    Srivastava, Kumkum
    Swain, Chris
    Tarnowski, Matthew J
    Thomson, Patrick
    Turner, Peter
    Wallace, Iain M
    Wells, Timothy NC
    White, Karen
    White, Laura
    Willis, Paul
    Winzeler, Elizabeth A
    Wittlin, Sergio
    Todd, Matthew H
    Griffith University Author(s)
    Duffy, Sandra
    Avery, Vicky M.
    Year published
    2016
    Metadata
    Show full item record
    Abstract
    The development of new antimalarial compounds remains a pivotal part of the strategy for malaria elimination. Recent large-scale phenotypic screens have provided a wealth of potential starting points for hit-to-lead campaigns. One such public set is explored, employing an open source research mechanism in which all data and ideas were shared in real time, anyone was able to participate, and patents were not sought. One chemical subseries was found to exhibit oral activity but contained a labile ester that could not be replaced without loss of activity, and the original hit exhibited remarkable sensitivity to minor structural ...
    View more >
    The development of new antimalarial compounds remains a pivotal part of the strategy for malaria elimination. Recent large-scale phenotypic screens have provided a wealth of potential starting points for hit-to-lead campaigns. One such public set is explored, employing an open source research mechanism in which all data and ideas were shared in real time, anyone was able to participate, and patents were not sought. One chemical subseries was found to exhibit oral activity but contained a labile ester that could not be replaced without loss of activity, and the original hit exhibited remarkable sensitivity to minor structural change. A second subseries displayed high potency, including activity within gametocyte and liver stage assays, but at the cost of low solubility. As an open source research project, unexplored avenues are clearly identified and may be explored further by the community; new findings may be cumulatively added to the present work.
    View less >
    Journal Title
    ACS Central Science
    Volume
    2
    Issue
    10
    DOI
    https://doi.org/10.1021/acscentsci.6b00086
    Copyright Statement
    © 2016 The Authors. This is an open access article published under a Creative Commons Attribution (CC-BY) License, which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited.
    Subject
    Chemical sciences
    Pharmacology and pharmaceutical sciences not elsewhere classified
    Publication URI
    http://hdl.handle.net/10072/124062
    Collection
    • Journal articles

    Footer

    Disclaimer

    • Privacy policy
    • Copyright matters
    • CRICOS Provider - 00233E
    • TEQSA: PRV12076

    Tagline

    • Gold Coast
    • Logan
    • Brisbane - Queensland, Australia
    First Peoples of Australia
    • Aboriginal
    • Torres Strait Islander